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| ID | PMID | YEAR | Sequence | Name | Length | N-ter MOD | C-ter MOD | Linear/Cyclic | Chirality | Chem-MOD | Origin | Nature | Incubation Time | Concentration | Half Life | Units Half Life | Protease | Assay | Test Sample | Vivo/Vitro | Reference | Patent No. | Activity |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 38917331 | 2024 | Aptamer-split peptide conjugate | 34 | DBCO modified S10 at C terminus | DBCO modified S11 peptide at N terminus | Linear | L | Azide-modified aptamer fragments (5 SSA and 3 SSA) "TTAATTCTGGGGGAGCCTTTTGTGGGTAGGGTTTTGTGGGTAGGGCGGGTTGGTTTTCGGGTTGGTTTTGCCCCGGAGGAGGAATT" are conjugated with DBCO-modified peptides (S10 and S11) , DBCO = Dibenzocyclooctyne | Aptamer-peptide complex | Hetero modulator for split GFP in response to ATP | Samples were collected every 24 h for 7 days | 1 μM | 4 | C57Bl/6N Mice serum protease | Serum stability assay | C57BL/6N Mice serum | In Vitro | None | None | A shorter antisense DNA of 11 nucleotides (aptamer) showed an EC50 value of 238 μM | |||
| 38807146 | 2024 | TG103 | 62 | Free | Fc region of IgG joined through (CH2-CH3) IgD | Linear | L | GLP-1 dimerization | GLP-1 analogs | Antiobesity | Blood sampling time points:(1) Within 2 h before dosing on day 1 and day 8,(2) 6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 15) after dosing on day 8 (3)Within 2 h before dosing on day 64, day 71 and day 78 (4)6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78. | 15.0 mg | 116 ± 10.8 (Terminal Half Life) | Human serum protease | Double-antibody sandwich assay | Human serum | In Vivo | None | None | N.A. | |||
| 38807146 | 2024 | TG103 | 62 | Free | Fc region of IgG joined through (CH2-CH3) IgD | Linear | L | GLP-1 dimerization | GLP-1 analogs | Antiobesity | Blood sampling time points:(1) Within 2 h before dosing on day 1, day 8 and day 15, (2) 6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 22) after dosing on day 15 (3)Within 2 h before dosing on day 64, day 71 and day 78 (4) 6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78. | 22.5 mg | 110 ± 11.9 (Terminal Half Life) | Human serum protease | Double-antibody sandwich assay | Human serum | In Vivo | None | None | N.A. | |||
| 38807146 | 2024 | TG103 | 62 | Free | Fc region of IgG joined through (CH2-CH3) IgD | Linear | L | GLP-1 dimerization | GLP-1 analogs | Antiobesity | Blood sampling time points: (1) Within 2 h before dosing on day 1, day 8, day 15 and day 22, (2)6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 29) after dosing on day 22,(3)Within 2 h before dosing on day 64, day 71 and day 78 (4) 6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78. | 30.0 mg | 116 ± 9.34 (Terminal Half Life) | Human serum protease | Double-antibody sandwich assay | Human serum | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Liraglutide | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 5.3 ± 1.5 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 0.5 ± 0.1 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38789061 | 2024 | Liraglutide | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Blood samples (250 μL) were collected at predetermined time points. For SC-dosed rats, time points included pre-dose, 15 min, 30 min, 1 hr, 2 hr, 3 hr, 4 hr, 8 hr, 10 hr, 24 hr, and 30 hr | 1 mg/kg | 9.1 ± 2.9 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 1.03 ± 0.10 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38789061 | 2024 | Liraglutide (Lymph cannulated) | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Lymph was collected continuously into tubes at specified time intervals: predose, 0–15 min, 15–30 min, 30 45 min, 45–60 min, 1–1.5 hr, 1.5–2 hr, 2–3 hr, 3–4 hr, 4–6 hr, 6–8 hr, 8–10 hr, 10–24 hr, and 24–30 hr | 2 mg/kg | 12.61 ± 5.45 | Male SD rats lymph protease | UHPLC | Male SD rats thoraic lymph | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide (Lymph cannulated) | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Lymph was collected continuously into tubes at specified time intervals: predose, 0–15 min, 15–30 min, 30 45 min, 45–60 min, 1–1.5 hr, 1.5–2 hr, 2–3 hr, 3–4 hr, 4–6 hr, 6–8 hr, 8–10 hr, 10–24 hr, and 24–30 hr | 1 mg/kg | 10.26 ± 6.51 | Male SD rats lymph protease | UHPLC | Male SD rats thoraic lymph | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 1 mg | 17.9 ± 2.1 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 3 mg | 21.3 ± 6.2 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 10 mg | 26.1 ± 7.0 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 20 mg | 35.4 ± 9.6 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 40 mg | 45.0 ± 13 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 80 mg | 52.5 ± 17 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides Therapy For Pv And Hemochromatosis | N.A. | 40 mg | 49.6 ± 18 | Human Plasma Protease | high-performance liquidchromatography–tandem mass spectrometry method | Human plasma after 2 once weekly repeated dose | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides Therapy For Pv And Hemochromatosis | N.A. | 40 mg | 36.1 ± 21 | Human Plasma Protease | high-performance liquidchromatography–tandem mass spectrometry method | Human plasma after 2 once weekly repeated dose | In Vivo | None | None | N.A. | |||
| 38737283 | 2024 | ABD035-immunoGN | N.A. | P1h3 | His-tag | Linear | L | Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N | Synthetic | Antitumor | Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min | 0.1 μmol/kg | 35.22 | BALB/c mice serum protease | ELISA | BALB/c mice serum | In Vivo | None | None | Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation | |||
| 38737283 | 2024 | immunoGN | N.A. | P1h3 | His-tag | Linear | L | Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N | Synthetic | Antitumor | Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min | 0.1 μmol/kg | 4.599 | BALB/c mice serum protease | ELISA | BALB/c mice serum | In Vivo | None | None | Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation | |||
| 38737283 | 2024 | dAb7h8-immunoGN | N.A. | P1h3 | His-tag | Linear | L | Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N | Synthetic | Antitumor | Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min | 0.1 μmol/kg | 31.25 | BALB/c mice serum protease | ELISA | BALB/c mice serum | In Vivo | None | None | Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 100 µg/kg | 8.43 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 30 µg/kg | 15.4 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 100 µg/kg | 7.36 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 300 µg/kg | 9.21 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.02 mg/kg | 32.3 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.007 mg/kg | 24 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.02 mg/kg | 24.3 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.07 mg/kg | 27.7 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38642503 | 2024 | VPALR-SUL | 5 | Free | Sul = Sulpiride | Linear | L | None | Derived from the Ku70 domain | Antidepressant | Blood samples were collected from the orbital venous plexus at various time points (5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 5 h, 7 h, 9 h, 12 h, 24 h | Equivalent of 3 mg/kg of sulpiride | 17.49 ± 13.50 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | VPALR-SUL showed almost 100% cell viability at all tested concentrations, which indicates excellent biocompatibility with HT22 nerve cells and minimal cytotoxicity | |||
| 38613996 | 2024 | PepH3 | 7 | Free | Amidation | Linear | L | None | Synthetic | Anticancer | At different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C | 1 mM | 21.00 ± 2.91 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | IC50 > 100.0 for TNBC MDA-MB-231 Monolayer | |||
| 38613996 | 2024 | vCPP2319 | 20 | Free | Amidation | Linear | L | None | Synthetic | Anticancer | At different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C | 1 mM | 280.40 ± 59.20 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | IC50 = 4.00±1.03 for TNBC MDA-MB-231 Monolayer | |||
| 38613996 | 2024 | PepH3-vCPP2319 5 | 27 | Free | Amidation | Linear | L | Ahx links two peptide | Synthetic chimeric peptide of PepH3 and vCPP2319 | Anticancer | At different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C | 1 mM | 125.20 ± 34.21 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | IC50 = 5.20±1.04 for TNBC MDA-MB-231 Monolayer | |||
| 38601038 | 2024 | DR10627 | 39 | Free | Amidation | Linear | L | A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position | GLP-1 analogs | Antiobesity, Antidiabetes | Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration | 1 nmol/kg | 5.80 ± 1.26 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action | |||
| 38601038 | 2024 | DR10627 | 39 | Free | Amidation | Linear | L | A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position | GLP-1 analogs | Antiobesity, Antidiabetes | Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration | 5 nmol/kg | 5.05 ± 0.405 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action | |||
| 38601038 | 2024 | DR10627 | 39 | Free | Amidation | Linear | L | A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position | GLP-1 analogs | Antiobesity, Antidiabetes | Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration | 26 nmol/kg | 4.19 ± 0.957 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action | |||
| 38555444 | 2024 | Aβ11/T80@CSs-TGC | 12 | Free | Linked with Chol using PEG2k linker | Linear | L | None | Synthetic | Treating intracranial infections caused by multidrug resistant Acinetobacter Baumannii | Blood samples were collected at predetermined time points (0.25, 0.5, 1, 2, 4, 6, and 8 h), | 12.5 mg/kg | 1.26 ± 0.21 | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | Both free TGC and Aβ11/T80@CSs-TGC displayed potent antimicrobial activity with a minimum inhibitory concentration of 2 μg/mL | |||
| 38554247 | 2024 | MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | None | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | 8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38554247 | 2024 | K2-MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | Alkyl chain conjugated with Lys2 side chain | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | Remained intact for 78.68% after 24 Hours | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38554247 | 2024 | K2-K4-MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | Alkyl chain conjugated with Lys2, Lys4 side chain | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | Remained intact for 75.61% after 24 Hours | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38493673 | 2024 | Peptide ALW | 12 | Free | Free | Linear | L | None | Synthetic | Alleviating Lupus Nephritis | N.A. | 12.5 mg/kg | 0.315 (Elimination Half Life) | Cd1 mice plasma protease | N.A. | CD1 mice plasma | In Vivo | None | None | KD(M) = 1.99*10-4 (Binding affinity of peptides to anti-dsDNA IgG3) | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼16.8 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38486997 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys20 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Attenuates Renal Fibrosis | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼8 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼20.5 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38486997 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys20 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Attenuates Renal Fibrosis | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼7.95 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | N.A. | 25.0 μg/kg | 84 | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | N.A. | 25.0 μg/kg | N.A. | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38399408 | 2024 | BI-X | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment Of Human Ocular Disease | serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals. | 0.25 mg/eye | 3 | Cynomolgus Monkeys Plasma Protease | Immunocapture-LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Affinity binding site to human albumin (KD = 1.4 nM) | |||
| 38399408 | 2024 | BI-X | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment Of Human Ocular Disease | serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals. | 0.25 mg/eye | 13.2 | Cynomolgus Monkeys Plasma Protease | Immunocapture-LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Affinity binding site to human albumin (KD = 1.4 nM) | |||
| 38399408 | 2024 | BI-X | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Treatment Of Human Ocular Disease | serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals. | 0.25 mg/eye | 11.8 | Cynomolgus Monkeys Plasma Protease | Immunocapture-LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Affinity binding site to human albumin (KD = 1.4 nM) | |||
| 38356317 | 2024 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety conjugated with Lys20, Aib modification at position 2,13 | GLP-1 analogs | Antidiabetes | PK samples were collected after single and multiple doses, up to 109 weeks of continuous tirzepatide treatment | 2–500 ng/mL. | 5.4 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38340726 | 2024 | A1L35HR2m | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Free | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | Sera were collected from these mice before (0 h) and 2, 4, 8, 12, 24, 48, 72, 120, 168, 240 and 336 h after injection | 5 mg/kg | 2.64 | Balb/c mice serum protease | N.A. | BALB/c mice serum | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | Sera were collected from these mice before (0 h) and 2, 4, 8, 12, 24, 48, 72, 120, 168, 240 and 336 h after injection | 5 mg/kg | 81.83 | Balb/c mice serum protease | N.A. | BALB/c mice serum | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 89.8 | Balb/c mice serum protease | N.A. | Balb/c mice lung tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 10.6 | Balb/c mice serum protease | N.A. | Balb/c mice trachea tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker, | Chol conjugation at C terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 49 | Balb/c mice serum protease | N.A. | Balb/c mice nose tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38312052 | 2024 | Maraciclatide (99mTc) | 7 | Acetylation | Free | Cyclic(Ac-Cys8 Bond, Cys2-Cys6 Disulfide Bond) | L | Radiolabelled with technetium, X= Unknown Structure | synthetic | Novel Diagnostic Imaging Agent For A Range Of Pathological Conditions | Blood and plasma samples were collected at 10 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, and 7 days post-administration | The data acquired from all participants who received 99mTc-maraciclatide within the expected clinical range (15, 75 µg, 150) were pooled | 1 (Terminal Elimination Half Life) | Human Plasma Protease | Gamma counter | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/73050806 | None | N.A. | |||
| 38293540 | 2024 | GLP-ABD-XTEN144 | 257 | GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tag | ABD was connected to the N-terminus of the XTEN polypeptide (144 amino acids) through a (GGGGS)3 linker | Linear | L | None | Fusion protein of GLP-1, ABD, XTEN (either 144 or 288) | Antidiabetes, Antiobesity | At 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein | 5 nmol | 12.9 | C57Bl/6 mice plasma protease And DPP-4 | ELISA | C57BL/6 mice plasma | In Vivo | None | None | GLP-ABD-XTEN144 has a Kd value of only 5.50 nM | |||
| 38293540 | 2024 | GLP-ABD-XTEN288 | 401 | GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tag | ABD was connected to the N-terminus of the XTEN polypeptide (288 amino acids) through a (GGGGS)3 linker | Linear | L | None | Fusion protein of GLP-1, ABD, XTEN (either 144 or 288) | Antidiabetes, Antiobesity | At 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein | 5 nmol | 7.32 | C57Bl/6 mice plasma protease And DPP-4 | ELISA | C57BL/6 mice plasma | In Vivo | None | None | GLP-ABD-XTEN288 showed a Kd value of 27.78 nM | |||
| 38236561 | 2024 | Cotadutide | 29 | Free | Free | Linear | L | palm-Glu-OH conjugated at Lys9 side chain | Synthetic | Dual GLP-1 and Glucagon (GCG) Receptor agonist | N.A. | 20 to 600 μg | 13.3 | N.A. | N.A. | N.A. | In Vivo | None | None | N.A. | |||
| 38104907 | 2024 | [Al18F]NODA-MPAA-HTA | 8 | Conjugating 18F nuclide with a modified KE108 peptide, MPAA modification at N terminal | The amino group of KE108 peptide conjugated with the carboxyl group of NODA | Cyclic(d-Dab2-Phe8) | Mix | D-Tryp amino acid substituition, d-Dab = Diaminobutyric acid | 18F-radiolabeled somatostatin analogue | Used for PET imaging of Neuroendocrine tumors (NETs) | Blood samples were collected from the retroorbital plexus into capillary at 5, 10, 15, 30,60 and 120 min | N.A. | 37.63 ± 13.05 (Elimination Half Life) | BALB/c mice blood protease | Gamma counter | BALB/c mice blood sample | In Vivo | None | None | Affinity of [Al18F]NODA-MPAA-HTA (Kd = 8.77 ± 1.14 nM, n = 4) | |||
| 38006944 | 2024 | Fatty Acid Modified TMP | 108 | Free | Free | Linear | L | C41H70O15N4 fatty acid modification | TMP analogue | Treatment of Thrombocytopenia | N.A. | 100 μg/kg | 128.5 | Beagle dogs plasma protease | ELISA | Beagle dogs plasma | In Vivo | None | None | The modified TMPs, particularly the C41H70O15N4 group, showed enhanced and prolonged activity, reaching peak platelet counts of 5047 × 10⁹/L at 216 hours (enhanced platelet counts) | |||
| 37818589 | 2024 | ΔTRTX-Ac1 | 28 | Free | Free | Cyclic (C2-C9-C18-C19-C22-C27 form LCK Loop) | L | None | From venom of the Mexican Blond tarantula spider Aphonopelma chalcodes | Antidiabetes | Blood withdrawn by cardiac puncture at0, 2, 4, 6, 8 and 12 h post-administration | 10 mg/kg | 2.17 | C57Bl/6 Male Mice Plasma Protease | Mass spectrometry | C57BL/6 male mice plasma | In Vivo | https://dom-pubs.pericles-prod.literatumonline.com/doi/10.1111/dom.15319 | None | The activity value of ΔTRTX-Ac1 alone shows minimal influence on reducing circulating glucose levels, with glucose levels remaining at 23.7 ± 3.1 mmol/L in high-fat-fed/streptozotocin (HFF/STZ) mice | |||
| 37818589 | 2024 | ΔTRTX-Ac1 | 28 | Free | Free | Cyclic (C2-C9-C18-C19-C22-C27 form LCK Loop) | L | None | From venom of the Mexican Blond tarantula spider Aphonopelma chalcodes | Antidiabetes | Blood withdrawn by cardiac puncture at 0, 2, 4, 6, 8 and 12 h post-administration | 10 mg/kg | 2.16 | C57Bl/6 Male Mice Pancreas Protease | Mass spectrometry | C57BL/6 male mice pancreas | In Vivo | https://dom-pubs.pericles-prod.literatumonline.com/doi/10.1111/dom.15319 | None | The activity value of ΔTRTX-Ac1 alone shows minimal influence on reducing circulating glucose levels, with glucose levels remaining at 23.7 ± 3.1 mmol/L in high-fat-fed/streptozotocin (HFF/STZ) mice | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 36 Hours | 4.06 nmol/kg | 68 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 386.4 nmol/kg | 64 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 350.4 nmol/kg | 77 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 352.5 nmol/kg | 76 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 375.7 nmol/kg | 46 | Dogs plasma protease | LC-MS | Dogs plasma after food is provided 1 min post dose | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 377.1 nmol/kg | 55 | Dogs plasma protease | LC-MS | Dogs plasma after food is provided 30 min post dose | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 2 | 40 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, aMeL13, Ornl6, K17, Aib20, D-Glu24, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.06 nmol/kg | 105 | Dogs plasma protease | LC-MS | Dogs plasma after food is provided 30 min post dose | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 2 | 40 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, aMeL13, Ornl6, K17, Aib20, D-Glu24, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 389 nmol/kg | 96 | Dogs plasma protease | LC-MS | Dogs plasma after treatment with Sodium Caprate (C10, 280Mg) | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 3 | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.01 nmol/kg | 104 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 3 | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 20 mg | 111 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 3 | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 20 mg | 104 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | TZP | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.15 nmol/kg | 70 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | TZP | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.15 nmol/kg | 159 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | TZP | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 20 mg | 97 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 0.1 mg/kg | 3.49 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 1 mg/kg | 3.34 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 10 mg/kg | 7.64 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 0.1 mg/kg | 18.8 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 1 mg/kg | 10 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 10 mg/kg | 10.2 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 8.4 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.33 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.66 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 14 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.11 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 14 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 7 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 8 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.67 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.85 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.8 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.16 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.31 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.04 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.68 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.83 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 6.59 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.66 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.01 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 5.7(Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.05 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.13 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.09 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.41 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 6 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.9 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 25 μg/kg | 0.79 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 50 μg/kg | 0.92 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 100μg/kg | 1.15 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 150 μg/kg | 1.15 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 50 μg/kg | 1.38 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 100μg/kg | 2.18 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 140 μg/kg | 1.94 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 200 μg/kg | 1.94 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 250 μg/kg | 1.88 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| 38863646 | 2024 | (89Zr, Mn)-WPMNs | N.A. | Free | Free | Linear | L | Mn and 89Zr labeling, MNPs modified with WL12-SH | WL12 derivative | Targets PD-L1 | Blood samples were collected from orbital vein at 1, 3, 5, 10, 15, 20, 30, 45 min and 1, 1.5, 2, 3, 4, 14, 24, 48, 72, 96 h | 0.5 mg/ml | 0.1234 (Fast) (Metabolic Half Life) | KM mouse blood protease | Radioactivity assay using γ-counter | KM mouse blood | In Vivo | None | None | N.A. | |||
| 38863646 | 2024 | (89Zr, Mn)-WPMNs | N.A. | Free | Free | Linear | L | Mn and 89Zr labeling, MNPs modified with WL12-SH | WL12 derivative | Targets PD-L1 | Blood samples were collected from orbital vein at 1, 3, 5, 10, 15, 20, 30, 45 min and 1, 1.5, 2, 3, 4, 14, 24, 48, 72, 96 h | 0.5 mg/ml | 1.554 (Slow) (Distribution Half Life) | KM mouse blood protease | Radioactivity assay using γ-counter | KM mouse blood sample | In Vivo | None | None | N.A. | |||
| 38697423 | 2024 | DAE Rum55 | N.A. | N.A. | N.A. | N.A. | D | N.A. | Ruminococcus sp. CAG55 | Epimerase | 50 °C | N.A. | 4.5 (Activity Half Life) | N.A. | N.A. | N.A. | In Vitro | None | None | D-allulose/D-psicose 3-epimerase (DAE/DPE, EC 5.1.3.30) and D-tagatose 3-epimerase (DTE, EC 5.1.3.31), of which DAE usually exhibits higher catalytic activity | |||
| 38697423 | 2024 | E268R-EKL16 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Ruminococcus sp. CAG55 derivative | Epimerase | 50 °C | N.A. | 135.3 (Activity Half Life) | N.A. | N.A. | N.A. | In Vitro | None | None | D-allulose/D-psicose 3-epimerase (DAE/DPE, EC 5.1.3.30) and D-tagatose 3-epimerase (DTE, EC 5.1.3.31), of which DAE usually exhibits higher catalytic activity | |||
| 38753095 | 2024 | Xyn10-HB | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | GH10 xylanase from Halalkalibacterium halodurans C-125 | GH10 xylanase | pH 8.5 and 60 °C | N.A. | 3 (Activity Half Life) | N.A. | N.A. | N.A. | In Vitro | None | None | Xyn10-HB produced active XOS with antioxidant activity determined by the DPPH radical scavenging method (IC50 of 0.54 mg/mL after 4 h) | |||
| 38115231 | 2024 | Trx1P | N.A. | N.A. | N.A. | Linear | L | N.A. | Derived from E. coli thioredoxin (Trx). | N.A. | N.A. | N.A. | 124 ± 15 (T1/2 Cis-Trans Isomerizations) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 38115231 | 2024 | Trx1Thp | N.A. | N.A. | N.A. | Linear | L | Incorporation of 4-thiaproline (Thp) at position cisPro76 | Derived from E. coli thioredoxin (Trx). | N.A. | N.A. | N.A. | 33 ± 3 (T1/2 Cis-Trans Isomerizations) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 37827496 | 2024 | TTRA81V heterozygous | 508 | N.A. | N.A. | Linear | L | Alanine (Ala) is substituted with valine (Val) at position 81 | Derived from missense mutation in the TTR gene | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 21 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 37827496 | 2024 | TTRA81V homozygous | 508 | N.A. | N.A. | Linear | L | Alanine (Ala) is substituted with valine (Val) at position 81 | Derived from missense mutation in the TTR gene | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 17.5 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 37827496 | 2024 | TTRWT (wild-type transthyretin) | 508 | N.A. | N.A. | Linear | L | None | Liver‐secreted plasma protein | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 44 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 37827496 | 2024 | TTRL55P mutation | 508 | N.A. | N.A. | Linear | L | leucine (Leu) is substituted with proline (Pro) at position 55 | Derived from missense mutation in the TTR gene (L55P) | Causes mild transthyretin amyloid cardiomyopathy | N.A. | 3.6 μM | 4.4 | Urea between 0.5 and 9 M in phosphate buffer (1 mM of EDTA, 10 mM of sodium phosphate, and 100 mM of potassium chloride, pH = 7.4 | UPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 4 μg/kg | 144 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 8 μg/kg | 147 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 14 μg/kg | 135 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 20 μg/kg | 147 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 40 μg/kg | 141 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 60 μg/kg | 154 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 100 μg/kg | 180 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 1 mg | 155.03 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 2 mg | 151.53 ( terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 4 mg | 155.85 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 8 mg | 159.95 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 12 mg | 170.62 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 16 mg | 161.76 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38952487 | 2024 | [3H]-semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H) | GLP-1 analogs | GLP-1 receptor agonist | Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose | 1 mg/ml | 168.3 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Intact [3H]-semaglutide-related material | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H), other metabolite may be attached | GLP-1 analogs | GLP-1 receptor agonist | Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose | 1 mg/ml | 201.2 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Dry [3H]-semaglutide-related material | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H), other metabolite may be attached | GLP-1 analogs | GLP-1 receptor agonist | Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose | 1 mg/ml | 180.5 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for PK assessment of semaglutide were taken at the following time points after the first dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144 and 168 h and at the following time points after the last dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h. Additional PK samples were taken before dosing in weeks 4, 8 and 11 | 0.5 mg | 156 | Human blood sample protease | LC-MS/MS | Human blood sample with once weekly dosage (at steady state) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for PK assessment of semaglutide were taken at the following time points after the first dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144 and 168 h and at the following time points after the last dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h. Additional PK samples were taken before dosing in weeks 4, 8 and 11 | 1 mg | 159 | Human blood sample protease | LC-MS/MS | Human blood sample with once weekly dosage (at steady state) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 183 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Normal Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 169 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Mild Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 201 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Moderate Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 221 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Severe Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | For ESRD subjects on hemodialysis, hourly blood samples were drawn during each of the first two hemodialysis sessions post-administration (each hemodialysis session lasted for ~2–4 h). | 0.5 mg | 243 (elimination half life) | Human serum protease | LC-MS/MS | Human serum dosage 1–24 H after hemodialysis, With No Hemodialysis For 48 H Post-Dose (End Stage Renal Disease Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 150 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Normal Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 155 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Mild Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 151 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Moderate Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 163 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Severe Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | N.A. | 20 mg | 153 | Human plasma protease | Luminescence oxygen channelling immunoassay (LOCI) | Human plasma dosed at steady state (Healthy) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | N.A. | 40 mg | 161 | Human plasma protease | Luminescence oxygen channelling immunoassay (LOCI) | Human plasma dosed at steady state (Healthy) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | N.A. | 40 mg | 158 | Human plasma protease | Luminescence oxygen channelling immunoassay (LOCI) | Human plasma dosed at steady state (Type 2 Diabetic) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | 10 days | 10 mg | 160 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 mg Once Daily Semaglutide (Subjects In The Fasting Arm Were Fasting Overnight For At Least 10 H Before Each Dosing) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | 10 days | 10 mg | 152 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 Mg Once Daily Semaglutide (Subjects In The Reference Arm Were Fasting Overnight For At Least 6 H Before Each Dosing) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for semaglutide PK assessment were drawn onday 1 (pre- and post-dose), then pre-dose on days 6 to 10 | 7 mg | 141 | Human plasma protease | N.A. | Human plasma (Type 2 Diabetic Patient With Upper Gastrointestinal Disease) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for semaglutide PK assessment were drawn onday 1 (pre- and post-dose), then pre-dose on days 6 to 10 | 7 mg | 142 | Human plasma protease | N.A. | Human plasma (Type 2 Diabetic Patient Without Upper Gastrointestinal Disease) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were drawn into K3EDTA tubes pre-dose on day 1, and at set time points on days 9 and 10 | 10 mg | 150 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 mg Semaglutide Once Daily For 5 Days | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were drawn into K3EDTA tubes pre-dose on day 1, and at set time points on days 9 and 10 | 10 mg | 156 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 mg Semaglutide Once Daily For 5 Days And With Omeprazole 40 Mg | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38116563 | 2023 | Ex-DARP-FGF21 | 327 | Exendin-4 peptide (Ex) fused to the N-terminus of the DARPin (DARP) protein via (GGGGS)3, His-tag and TEV protease site introduced at position 1 | FGF21 fused to the C-terminus of the DARPin (DARP) protein via (GGGGS)3 linker | Linear | L | L98R and P171A amino acid substitutions in FBGF21 | Exendin-4, DARPin, FGF21 fusion protein | Antidiabetes, Antiobesity | Approximately 40 µL of blood was collected from the orbital venous plexus at different time points (1, 3, 8, 12, 24, 36, 48, and 72 h) | 10 nmol/kg | 27.6 ± 3.2 | C57BL/6 mice plasma protease | ELISA | C57BL/6 mice plasma | In Vivo | None | None | Ex-DARP-FGF21 and Ex-DARP were efficaciously bound to HSA with half-maximal binding concentrations of 4.5 nM and 1.9 nM, respectively | |||
| 38097378 | 2023 | Au_CR | 2 | Au gold particle conjuagtion at N terminal through formation of Au-S bond | Amidation | Linear | L | None | Synthetic | Antimicrobial | Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h | 10 mg/kg | ∼17.5 | Mice plasma protease | ICP-MS | Mice plasma | In Vivo | None | None | MIC(μg/mL) = 1.56 against S. aureus | |||
| 38097378 | 2023 | Au_CR | 2 | Au gold particle conjuagtion at N terminal through formation of Au-S bond | Amidation | Linear | L | None | Synthetic | Antimicrobial | Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h | 10 mg/kg | ∼17.5 | Mice plasma protease | ICP-MS | Mice plasma | In Vivo | None | None | MIC(μg/mL) >100 against E.coli | |||
| 38097378 | 2023 | Au_CR | 2 | Au gold particle conjuagtion at N terminal through formation of Au-S bond | Amidation | Linear | L | None | Synthetic | Antimicrobial | Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h | 10 mg/kg | ∼17.5 | Mice plasma protease | ICP-MS | Mice plasma | In Vivo | None | None | MIC(μg/mL) >100 against B.subtilis | |||
| 38097378 | 2023 | Au_CR | 2 | Au gold particle conjuagtion at N terminal through formation of Au-S bond | Amidation | Linear | L | None | Synthetic | Antimicrobial | Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h | 10 mg/kg | ∼17.5 | Mice plasma protease | ICP-MS | Mice plasma | In Vivo | None | None | MIC(μg/mL) = 1.56 against C.albicans | |||
| 38092894 | 2023 | Tag-free rhMFG-E8 | 387 | 23 amino acid leader sequence of cystatin S introduced at N terminal | Free | Linear | L | None | Expressed in Expi293F cells | Antiinflammatory (Including Radiation Injury) | Blood samples (100 μl per time point) were collected starting from 2 to 6 hours | 50 µg | 1.45 (Terminal Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The tag-free rhMFG-E8 demonstrated markedly higher cell adhesion binding activity (to SVEC4-10 cells) compared to E. coli-expressed His-tagged rhMFG-E8, which binds to αVβ3 integrin on the membrane of phagocytes | |||
| 38092894 | 2023 | Tag-free rhMFG-E8 | 387 | 23 amino acid leader sequence of cystatin S introduced at N terminal | Free | Linear | L | None | Expressed in Expi293F cells | Antiinflammatory (Including Radiation Injury) | Blood samples (100 μl per time point) were collected starting from 2 to 12 hours | 50 µg | 2.33 (Terminal Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The tag-free rhMFG-E8 demonstrated markedly higher cell adhesion binding activity (to SVEC4-10 cells) compared to E. coli-expressed His-tagged rhMFG-E8, which binds to αVβ3 integrin on the membrane of phagocytes | |||
| 38027063 | 2023 | ScFv9-CD | 466 | Free | Fusion of CD | Linear | L | Biotinylation | CD sequence originates from the C1qTNF3 protein and scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ) | Treatment of AD and Parkinson disease | Plasma was collected at 0, 2, 4, 8, and 24 h after injection | 250 μg | 1.82 | TgCRND8 mice plasma protease | Direct ELISA | TgCRND8 mice plasma | In Vivo | None | None | N.A. | |||
| 38027063 | 2023 | ScFv9 | 304 | Free | Free | Linear | L | Biotinylation | The scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ) | Treatment of AD and Parkinson disease | Plasma was collected at 0, 2, 4, 8, and 24 h after injection | 250 μg | 0.74 | TgCRND8 mice plasma protease | Direct ELISA | TgCRND8 mice plasma | In Vivo | None | None | N.A. | |||
| 37880318 | 2023 | L1 | 15 | Acetylation | Free | Linear | L | None | Derived from calcitermin | Antimicrobial | 37 °C | 0.0001 M | >2 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 40 ± 10 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation) | |||
| 37880318 | 2023 | L2 | 15 | Acetylation | Amidation | Linear | L | None | Derived from calcitermin | Antimicrobial | 37 °C | 0.0001 M | 68 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 211 ± 25 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation) | |||
| 37880318 | 2023 | L3 | 15 | Free | Amidation | Linear | L | None | Derived from calcitermin | Antimicrobial | 37 °C | 0.0001 M | 20 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 189 ± 23 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation) | |||
| 37880318 | 2023 | Wild-type Calcitermin (WT) | 15 | Free | Free | Linear | L | None | C-terminal cleavage fragment of calgranulin C | Antimicrobial | 37 °C | 0.0001 M | 18 ± 3 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 28 ± 15 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation) | |||
| 37875481 | 2023 | IL-15-Cy7 | N.A. | Free | Free | Linear | L | Cy7 | Derived from Interleukin-15 | Antitumor | The blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h) | N.A. | 0.69 | Mice blood protease | Fluorescence spectrophotometry | Mice blood | In Vivo | None | None | Not mentioned | |||
| 37875481 | 2023 | biNV-IL-15-Cy7 | N.A. | Free | Free | Linear | L | Cy7 | Derived from Interleukin-15 | Antitumor | The blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h) | N.A. | 5.66 | Mice blood protease | Fluorescence spectrophotometry | Mice blood | In Vivo | None | None | Not mentioned | |||
| 37874823 | 2023 | MDK1472 | 42 | Acetylation | Free | Cyclic (Disulphide Bond Bw C7-C16, C32-C41) | L | IL-7Ra binding domain linked with yc binding domain with the help of linker GGS linker | Synthetic | IL-7R agonist peptide | 37 °C | 10 mM | 60 | Human Plasma Protease | LC-MS/MS | Human plasma | In Vitro | None | None | IC50(nM) = 340 (IC50 values in a competition ELISA for compound binding to human IL-7Rα) | |||
| 37874823 | 2023 | MDK1472 | 42 | Acetylation | Free | Cyclic (Disulphide Bond Bw C7-C16, C32-C41) | L | IL-7Ra binding domain linked with yc binding domain with the help of linker GGS linker | Synthetic | IL-7R agonist peptide | 37 °C | 10 mM | 104 | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vitro | None | None | IC50(nM) = 190 (IC50 values in a competition ELISA for compound binding to Cyno IL-7Rα) | |||
| 37874823 | 2023 | MDK-703 | 110 | Fused with IgG2 Fc chain via (Gly-Ser)10 linker, Fc-fragments consisting of the CH2 and CH3 domains of the heavy chain and hinge regions of human IgG2 Fc modified as follows: The first and second cysteines of the hinge region were replaced with serine to prevent detrimental disulfide bridge formation; the last amino acid (lysine) of the Fc region was replaced with an alanine | Free | Linear | L | None | Synthetic | IL-7R agonist peptide | Blood samples were collected at pre-Dose (day 1), 0.5, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, and 216 h post-dose | 1 mg/kg | 46 (Terminal Half Life) | Cynomolgus monkeys serum protease | Sandwich ELISA | Cynomolgus monkeys serum | In Vivo | None | None | IC50(nM) = 190 (IC50 values in a competition ELISA for compound binding to Cyno IL-7Rα) | |||
| 37835489 | 2023 | QQT*-IRDye800 | 12 | QQT* conjugated with IRDye800 at C terminus using linker | Free | Linear | L | None | Synthetic | Used for in vivo imaging to identify premalignant Colorectal Lesions | RP-HPLC was performed at 0, 0.5, 1, 2, 4, 8, and 24 h | 30 μM | 3.6 | APC mice serum protease | RP-HPLC | APC mice serum | In Vivo | None | None | Not mentioned | |||
| 37759683 | 2023 | IBP-EK1 | 32 | Conjugation with human immunoglobulin G Fc-binding peptide (IBP) at n terminus | Free | Linear | L | None | Fusion protein | Antiviral | Serial blood samples were collected from monkeys that received IBP-EK1 or EK1 before injection and at 2, 4, 6, 24, 72, and 144 h post injection | 10 mg/kg | 37.67 | Rhesus monkeys serum protease | HPLC-MS/MS | Rhesus monkeys serum | In Vivo | None | None | IC50 = 788 nM for IBP-EK1 ( against Pseudotyped SARS-CoV-2 Variants on Caco-2 Cells) | |||
| 37759683 | 2023 | IBP-EK1 | 32 | Conjugation with human immunoglobulin G Fc-binding peptide (IBP) at n terminus | Free | Linear | L | None | Fusion protein | Antiviral | Serial blood samples were collected from monkeys that received IBP-EK1 or EK1 before injection and at 2, 4, 6, 24, 72, and 144 h post injection | 10 mg/kg | 39.72 | Rhesus monkeys serum protease | HPLC-MS/MS | Rhesus monkeys serum | In Vivo | None | None | IC50 = 788 nM for IBP-EK1 ( against Pseudotyped SARS-CoV-2 Variants on Caco-2 Cells) | |||
| 37449781 | 2023 | NCL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h | 5 μg/μL | 11.4 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 37449781 | 2023 | 2F-CL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h | 5 μg/μL | 11.3 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 37449781 | 2023 | 3F-CL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h | 5 μg/μL | 19.1 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 37397495 | 2023 | Peptide | 9 | Free | Free | Linear | L | Removing an Asp residue | Isolated from Merluccius productus fish protein hydrolysate | Inhibits BACE-1 | Blood was taken after 0, 5, and 30 min and 2, 6, and 24 h after injectio | 4 mg/kg | 0.69 | Mouse plasma protease | Mass spectrometry | Mouse plasma | In Vivo | None | None | Ki(µM)= 0.0940 BACE-1 activity with peptide which has reduced activity due to inhibition by peptide | |||
| 37390979 | 2023 | BI-3434 | 33 | Free | Amidation | Linear | L | Lys33 conjuagted with HLE (fatty acid based half life extension group),Substituting Ser with 2-aminoisobutyric acid (Aib) at position 2 | Lipidated secretin analog | Secretin receptor agonist | N.A. | 30 nmol/kg | <15 | Male NMRI mice plasma protease | Mass spectrometry | Male NMRI mice plasma (Non fasted) | In Vivo | None | None | EC50 =15.5 pM for BI-3434 | |||
| 37390979 | 2023 | Stapled secretin | 27 | Free | Amidation | Cyclic (E16-K20 Lactam Bridge) | L | E16, K20 modification | Human secretin modified analog | Secretin receptor agonist | N.A. | 30 nmol/kg | N.A. | Male NMRI mice plasma protease | Mass spectrometry | Male NMRI mice plasma (Non fasted) | In Vivo | None | None | EC50 = 1172 nM for native secretin on murine adipocytes | |||
| 37384895 | 2023 | CLA-coated PTX-SPIONs@HRH | 12 | Free | Free | Linear | L | None | Synthetic | Antiangiogenic (used for targeted delivery of Paclitaxel in non-small cell lung carcinoma) | Mice were euthanized over 24 h at t = 0.5, 1, 4, 8, and 24 h | 15.6 μg/mL | 17.1 | Mice Plasma Protease | HPLC | Mice plasma | In Vivo | None | None | The activity value for CLA-coated PTX-SPIONs@HRH at the maximal therapeutic concentration (100 μg/mL) resulted in 12.8% cell viability on A549 lung adenocarcinoma cells | |||
| 37384895 | 2023 | CLA-coated PTX-SPIONs@HRH | 12 | Free | Free | Linear | L | None | Synthetic | Antiangiogenic (used for targeted delivery of Paclitaxel in non-small cell lung carcinoma) | Mice were euthanized over 24 h at t = 0.5, 1, 4, 8, and 24 h | 15.6 μg/mL | 17.1 | Mice Plasma Protease | HPLC | Mice plasma | In Vivo | None | None | The activity value for CLA-coated PTX-SPIONs@HRH at the maximal therapeutic concentration (100 μg/mL) resulted in 12.8% cell viability on A549 lung adenocarcinoma cells | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 164 | Human plasma protease | Triple Quadrupole Mass spectrometry | Human plasma | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 82.5 | SD rats plasma protease | Triple Quadrupole Mass spectrometry | SD rats plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 54.6 | Beagle dogs plasma protease | Triple Quadrupole Mass spectrometry | Beagle dogs plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 52.7 | Cynomolgus monkeys plasma protease | Triple Quadrupole Mass spectrometry | Cynomolgus monkeys plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 5.68 | CD-1 mouse plasma protease | Triple Quadrupole Mass spectrometry | CD-1 mouse plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | 372 | Gastric fluid protease | Triple Quadrupole Mass spectrometry | Simulated Gastric Fluid (SGF) at pH = 1.3 | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | 2.72 | Intestinal fluid protease | Triple Quadrupole Mass spectrometry | Simulated Intestinal Fluid (SIF) at pH = 5.5 | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | >120 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 1.3 (acidic) | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | >120 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 5.5 (slightly acidic) | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | 433 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 7.4 (basic) | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 32.5 | CD-1 mouse Liver Microsomes protease | LC-MS/MS | CD-1 mouse Liver Microsomes | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 27.7 | SD rats Liver Microsome Protease | LC-MS/MS | SD rats Liver Microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 33 | Beagle dogs Liver Microsome Protease | LC-MS/MS | Beagle dogs Liver Microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 21.8 | Cynomolgus monkeys Liver Microsome Protease | LC-MS/MS | Cynomolgus monkeys Liver microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 20.3 | Human Liver Microsome protease | LC-MS/MS | Human Liver Microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | <15 | CD-1 mouse Hepatocytes Lysate Protease | LC-MS/MS | CD-1 mouse Hepatocytes Lysate | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.81 | SD rats Hepatocytes Lysates protease | LC-MS/MS | SD rats hepatocytes Lysates | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 10.7 | Beagle dogs Hepatocytes Lysates protease | LC-MS/MS | Beagle dogs Hepatocytes Lysates | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 12.1 | Cynomolgus monkeys Hepatocytes Lysates protease | LC-MS/MS | Cynomolgus monkeys Hepatocytes Lysates | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.28 | Human Hepatocytes Lysates protease | LC-MS/MS | Human Hepatocytes | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.28 | Human Hepatocytes Lysates protease | LC-MS/MS | Human Hepatocytes Lysates | In Vitro | None | None | Enzyme Activity = 3.18 at 2 microMolar of HM1010 (Cytochrome P450 (CYP2B6) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.28 | Human Hepatocytes Lysates protease | LC-MS/MS | Human Hepatocytes Lysates | In Vitro | None | None | Enzyme Activity = 2.06 at 2 microMolar of HM1010 (Cytochrome P450 (CYP3A4) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37094132 | 2023 | SNIO–CBP | 16 | Single nanometer iron oxide and PEG conjugation at N terminal | Amidation | Cyclic (C5-C14 Disulfide Bond) | L | None | SINO-CBP product | Used in detection of Liver Fibrosis | N.A. | 2 nmol/g animal | 5.7 ± 1.9 (Elimination Half Life) | Mice blood protease | Dynamic T1-weighted MRI | Mice blood | In Vivo | None | None | Kd = 18.4 µM (Binding affinity of SNIO–CBP toward human type I collagen) | |||
| 37073494 | 2023 | Carmo‐HrTH‐I | 10 | pGlu = Pyroglutamate | Amidation | Linear | L | C‐mannosylated tryptophan residue at position 8 | Derived from the corpora cardiaca (CC) of the Indian stick insect Carausius morosus | Hypertrehalosemia In Ligated Stick Insects | 0, 2‐, 5‐, 10‐and 30 min at Room temp | 100 pmol | 5 | C.Morosus hemolymph protease | HPLC | C.Morosus hemolymph | In Vitro | None | None | [Lipid]T0 min(µg/µL) = 9.32 ± 1.59 for Natural Carmo‐HrTH‐I (10 pmol) (Biological activity of a crude methanolic extract of corpora cardiaca (CC) from the natural hypertrehalosemic hormones (HrTHs) extracted from the CC of the Indian stick insect(Carausius morosus) in an in vivo bioassay withL. migratoria) | |||
| 37047588 | 2023 | B7-33 | 27 | Free | Free | Linear | L | None | Derived as a single-chain peptidomimetic of the B-chain of H2 relaxin | Treatment of Acute Cardiac Failure | A total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min) | 400 µg/mL | 6 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | HEK-7BP Binding B.S.A. Free Eu-H2 pKi = 7.28 ± 0.11 | |||
| 37047588 | 2023 | AcK(PalmGlu)-PEG12-B7-33 | 27 | Ac modifed Lysine in Palmitic fatty acid linked with B7-33 using PEG linker | Free | Linear | L | None | B7-33 analog | Treatment of Acute Cardiac Failure | A total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min) | 400 µg/mL | 60 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | HEK-7BP Binding B.S.A. Free Eu-H2 pKi =7.52 ± 0.13 | |||
| 36989942 | 2023 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys20 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes, Antiobesity | N.A. | N.A. | 7.22 - 9.26 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | PubChem CID: 56843331 | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1.5 mg/kg | 0.306 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 4.5 mg/kg | 0.344 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 13.5 mg/kg | 0.547 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.805 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.248 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.46 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.437 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.341 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.391 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.665 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.668 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.655 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.648 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.615 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.62 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.888 | Monkeys Plasma Protease | LC-MS/MS | Monkeys plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 50 mg/kg | 0.956 | Monkeys Plasma Protease | LC-MS/MS | Monkeys plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | 1 day | 3.2 mg/kg | 1.956 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | plasma samples were collected from patients before the CEND-1 infusion and at 3 min (±1 min), 15 min (±3 min), 30 min (±3 min), 1 hour (±5 min), ¾ h (±10 min) and 6/8 h (±10 min) after completion of the infusion (cycle 1 day 1 of nab-paclitaxel+gemcitabine chemotherapy treatment) (Combination therapy after 7 days of run in therapy) | 3.2 mg/kg | 1.725 | Human plasma protease | N.A. | Human plasma after nab-paclitaxel and gemcitabine | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | plasma samples were collected from patients before the CEND-1 infusion and at 3 min (±1 min), 15 min (±3 min), 30 min (±3 min), 1 hour (±5 min), ¾ h (±10 min) and 6/8 h (±10 min) after completion of the infusion (cycle 1 day 1 of nab-paclitaxel+gemcitabine chemotherapy treatment) (Combination therapy after 7 days of run in therapy) | 3.2 mg/kg | 1.598 | Human plasma protease | LC-MS/MS | Human plasma after nab-paclitaxel and gemcitabine | In Vivo | None | None | N.A. | |||
| 36902021 | 2023 | PDC | 16 | Free | PEG4 spacer was designed and subsequently reacted with a cysteine at the carboxyl terminus then, the elongated thiol-modified homodimer peptide was conjugated with DOX | Linear | L | None | HER2-targeting peptide–DOX conjugate | Antitumor | The PDC was incubated with human plasma (final peptide concentration of 50 μM) for 0, 2, 4, 8, 12, 24, and 48 h | 50 μM | 24 | Human plasma protease | HPLC | Human plasma | In Vitro | None | None | The IC50 value for the PDC (Peptide-Drug Conjugate) is 140 nM. This value indicates that the PDC is more potent in killing HER2-positive SKBR-3 cells compared to free DOX, which has an IC50 of 410 nM | |||
| 36873181 | 2023 | DR3penA | 8 | Free | Amidation | Linear | L | α-(4-pentenyl)-Ala introduced at positions 3 of DR8 | DR8 analog | Alleviates Pulmonary Fibrosis | Samples were taken from the mixture at 0, 15, 30, 60, 120 and 240 min | 10 mmol/L | 174.63 ± 31.66 | Mice serum protease | RP-HPLC | C57BL/6 mice serum | In Vitro | None | None | DR3penA has Minimum effective concentration is 2.5 μmol/L in both TGF-β1-induced NIH3T3 cells and A549 cells | |||
| 36873181 | 2023 | DR4penA | 8 | Free | Amidation | Linear | L | α-(4-pentenyl)-Ala introduced at positions 4 of DR8 | DR8 analog | Alleviates Pulmonary Fibrosis | Samples were taken from the mixture at 0, 15, 30, 60, 120 and 240 min | 10 mmol/L | 270.65 ± 16.43 | Mice serum protease | RP-HPLC | C57BL/6 mice serum | In Vitro | None | None | DR8 has Minimum effective concentrations are 20 μmol/L in TGF-β1-induced NIH3T3 cells and 10 μmol/L in A549 cells | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 200 nmol/kg | 36.4 (Terminal Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC 50 (nM) = 109 ± 24 of LY3540378 in Rat RXFP2 | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 100 nmol/kg | 124 (Terminal Half Life) | Cynomolgus monkeys plasma protease | LC-MS | Cynomolgus monkeys plasma | In Vivo | None | None | EC 50 (nM) = 19.3 ± 4.0 of LY3540378 in Cynomolgus monkey RXFP2 | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 100 nmol/kg | 45.7 (Terminal Half Life) | Cynomolgus monkeys plasma protease | LC-MS | Cynomolgus monkeys plasma | In Vivo | None | None | EC 50 (nM) = 19.3 ± 4.0 of LY3540378 in Cynomolgus monkey RXFP2 | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 30 nmol/kg | 39.7 ± 1.8 (Terminal Half Life) | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | None | EC 50 (nM) = 109 ± 24 of LY3540378 in Rat RXFP2 | |||
| 36780786 | 2023 | hGLP-2 (variant 6) | 33 | Free | Free | Linear | L | Addition of a C16 monoacid at position 20 of the hGLP-2 peptide | Proglucagon-derived intestinal hormone | Antiapoptosis, Antiinflammatory | Blood samples were drawn from the tail at t = 0.5, 1, 2, 4, 8, 12, 24, 36, and 48 h | 400 µg/kg | 9.5 | Female SD rats plasma protease | RIA | Female SD rats plasma | In Vivo | None | None | EC50 = 0.44 nM for hGLP-2R in the presence of 1% HSA | |||
| 36719326 | 2023 | 68Ga(AAZ3A-endoHB)-c(RGD) | 5 | Ga labelling, conjugation of AAZ3A-endoHB-NCS to c(RGD)(cyclo(Arg-Gly-Asp-D-Phe-Lys) peptide at N terminus | Free | Cyclic (RGDfK) | Mix | None | Synthetic | Positron Emission Tomography (PET) imaging | 37 °C | N.A. | Stable upto 4 hour | Human serum protease | UPLC-UV-RA | Human serum | In Vitro | None | None | N.A. | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | (Onc72 in 19% MHB2 medium) MIC = 12.5 μmol L−1 (29 mg L−1) on E.coli BW25113 | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | (Onc72 in 25% mouse serum ) MIC = 25 μmol L−1 (58 mg L−1) on E.coli BW25113 | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | Onc72 Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | Onc72: Non-toxic to human HepG2 and HEK293 cell lines at 50 μmol L−1 | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 66 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | (Prodrugs of Onc72) MIC values >50 μmol L−1 on E.coli BW25113 | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 66 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | Prodrugs Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 66 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | 5 kDa thiol-PEG: Reduced cell viability to ≈89% for both HepG2 and HEK293 cell lines | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | (Prodrugs of Onc72) MIC values >50 μmol L−1 on E.coli BW25113 | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | Prodrugs Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | 20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Synthetic | Antimicrobial | Aliquots weretaken in triplicates after 0, 1, 2, 4, and 8 h for Onc72 and 0, 4, 8, and 24 hfor both prodrugs | 31.5 μmol/L | ≈80 | Cell lysate protease (Obtained From An E. Coli Bw25113 Culture) | RP-HPLC | E. coli BW25113 cell lysate | In Vitro | None | None | (Onc72 in 19% MHB2 medium) MIC = 12.5 μmol L−1 (29 mg L−1) on E.coli BW25113 | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Synthetic | Antimicrobial | 0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates | 31.5 μmol/L | 8 | Mouse serum protease | Serum stability assay | Mouse serum | In Vivo | None | None | 5 kDa thiol-PEG: Reduced cell viability to ≈89% for both HepG2 and HEK293 cell lines | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Synthetic | Antimicrobial | 0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates | 31.5 μmol/L | 14 | Mouse serum protease | Serum stability assay | Mouse serum | In Vivo | None | None | 20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines | |||
| 36630826 | 2023 | Exendin-4 | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 2.12 ± 0.3 (T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36630826 | 2023 | Ex-PEGRh(4.4 ± 1.1nm) | 39 | Free | PEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 23.14 ± 3.2(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-PEGMw(46.3KDa) | 39 | Free | PEGylation (Mw(46.3KDa)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 34.91 ± 4.5(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 = 2.7 ± 0.5 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 97.3 ± 3.2(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Exendin-4 | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 1.88 ± 0.2(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36630826 | 2023 | Ex-PEGRh(4.4 ± 1.1nm) | 39 | Free | PEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 11.9 ± 2.7 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 12.1 ± 1.0 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 105.7 ± 6 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36595440 | 2023 | TP0597850 (18) | 4 | Tripeptide linker {5-aminopentanoic acid [Ape(5)]–Glu–Asp} of 1 was replaced by a shorter linker (γ-D-Glu), X = Structure given in paper | Free | Linear | L | X=Structure given in paper | Synthetic | MMP2 Inhibitors | N.A. | N.A. | 265 | N.A. | N.A. | N.A. | N.A. | None | None | Ki = 0.034 nM for MM2 inhibition | |||
| 36509220 | 2023 | KM8 | 18 | Free | Amidation | Linear | L | None | Analogue of Mastoparan | Antitumor | N.A. | N.A. | 30 | Mouse plasma protease | Plasma stability assay | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36410792 | 2023 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Small Bowel Hypertrophic Effect | Blood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912 | 670 nmol/kg | 0.6 ± 0.1 | SD rats serum protease | GLP-2 ELISA | SD rats serum | In Vivo | None | None | EC50 = 0.12 ± 0.056 nM for teduglutide peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP) | |||
| 36410792 | 2023 | HM15912 | 34 | [(1H-imidazol-4-yl)-acetyl 1] | Conjugation of GT15912 and hIgG4 Fc was carried out through the formation of amine bonds between the bi functional PEG and Lys34 in GT15912 or the N-terminal amino acid in hIgG4 Fc | Linear | L | None | GLP-2 analogue | Small Bowel Hypertrophic Effect | Blood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912 | 13 nmol/kg | 42.3 ± 3.4 | SD rats serum protease | GLP-2 ELISA | SD rats serum | In Vivo | None | None | EC50 = 0.327 ± 0.096 nM for HM15912 peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP) | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 2.12 ± 0.3 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 23.14 ± 3.2 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-PEGMw | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(46.3 KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 34.91 ± 4.5 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 (nM) = 2.7 ± 0.5 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional POEGMA(54.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 97.3 ± 3.2 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 (nM) = 2.8 ± 0.7 | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 1.88 ± 0.2 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 11.9 ± 2.7 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional POEGMA(54.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 105.7 ± 6 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 (nM) = 2.8 ± 0.7 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, And 48 H post I.V. application | 0.25 mg/kg | 7.9 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 8.21 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 7.33 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 5.69 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 8.68 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2.0 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 10.3 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2.0 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 6.19 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 6.97 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 11.2 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 9.7 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 11.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 10.8 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 19.6 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 20.1 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | SEQ ID NO 21 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 12.9 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.8 | |||
| N.A. | 2023 | SEQ ID NO 21 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 12.1 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.8 | |||
| N.A. | 2023 | SEQ ID NO 22 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 13.6 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 1 | |||
| N.A. | 2023 | SEQ ID NO 22 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 15.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 1 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 14.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 14.3 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0 H and after 0.083, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, 48, 56, 72, 80, and 96 H post I.V. application | 0.05 mg/kg | 64.1 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0 H and after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, 48, 56, 72, 80, and 96 H post S.C. application | 0.1 mg/kg | N.A. | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | RTD-1 | 16 | Free | Free | Linear | L | None | Theta Defensin | Antimicrobial | Blood samples were collected at 0.25, 1, 2, 4, 8, and 24 H post-dose via terminal cardiac puncture | 5 mg/kg | 6.05 (Elimination Half Life) | Mouse plasma protease | LC-MS with reverse phase liquid chromatography | Mouse plasma | In Vivo | None | US 2022/0048569 W | Administering an effective amount of the effective 9-defensin or the effective 0-dcfcnsin analog to the individual in need of treatment, wherein the effective amount provides antimicrobial activity directed to the microbe | |||
| N.A. | 2023 | SEQ ID NO 1 | 28 | Free | Free | Linear | L | None | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 0.2 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 0.83 | |||
| N.A. | 2023 | SEQ ID NO 2 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >19 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 1.9 | |||
| N.A. | 2023 | SEQ ID NO 23 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 103 | |||
| N.A. | 2023 | SEQ ID NO 24 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 54.5 | |||
| N.A. | 2023 | SEQ ID NO 25 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, NMeS = N-Methyl-L-Serine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 17 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 70.5 | |||
| N.A. | 2023 | SEQ ID NO 26 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, Deg = Di-ethyl glycine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 138 | |||
| N.A. | 2023 | SEQ ID NO 27 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, Tie = L-te/t-butyl-glycine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 61.8 | |||
| N.A. | 2023 | SEQ ID NO 28 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, Aib = 2-aminoisobutyric acid at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 72.4 | |||
| N.A. | 2023 | SEQ ID NO 29 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 36.6 | |||
| N.A. | 2023 | SEQ ID NO 30 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 56.5 | |||
| N.A. | 2023 | SEQ ID NO 31 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, NMeS = N- methyl-L-serine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 12 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 50.3 | |||
| N.A. | 2023 | SEQ ID NO 32 | 28 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 142 | |||
| N.A. | 2023 | SEQ ID NO 33 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, 1Nal = 3-(l-naphthyl)-L-alanine at position 4 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 61 | |||
| N.A. | 2023 | SEQ ID NO 34 | 29 | Free | Free | Linear | L | NMeS = N- methyl-L-serineat position 2,X = Octanoyl-Dpr at position 3, Nal = 3-(l-naphthyl)-L-alanine at position 4 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 25 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 27.2 | |||
| N.A. | 2023 | SEQ ID NO 35 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 63 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 76.7 | |||
| N.A. | 2023 | SEQ ID NO 36 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 44.5 | |||
| N.A. | 2023 | SEQ ID NO 37 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 27.5 | |||
| N.A. | 2023 | SEQ ID NO 38 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 56.1 | |||
| N.A. | 2023 | Parent compound 1 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 8 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 104 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 2.1 | |||
| N.A. | 2023 | Parent compound 3 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 131 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4 | |||
| N.A. | 2023 | Parent compound 4 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 56 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4.2 | |||
| N.A. | 2023 | Parent compound 5 | 39 | Free | Amidation | Linear | L | Aib at position 2 and 13, Chem.16[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19- carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 134 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 9.7 | |||
| N.A. | 2023 | Non-converting compound 1 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Aib at position 4, Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.8 mg | 137 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 2 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Aib at position 4,Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.5 mg | 130 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 3 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 , | Free | Linear | L | Aib at position 4,Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys 16 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 115 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 4 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl attached to Lys1 | Amidation | Linear | L | Aib at position 4,Chem. 11[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19-carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys20 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 136 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 1 | 41 | D-Lys conjugated with [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] | Free | Linear | Mix | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 , Sar2, Aib modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.1 mg | 146 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 2 | 41 | Free | Free | Linear | L | Aeg = N-(2-aminoethyl)glycine, Chem.16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Aeg2, Chem.8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 142 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 3 | 41 | Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modification | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 139 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 5 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to L-Aeg | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.8 mg | 106 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 12 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modfications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.7 mg | 143 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 13 | 41 | Chem. 17[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.8 mg | 121 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 14 | 41 | Chem. 22[(2S)-2,6-bis[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl] attached to Lys1 | Free | Linear | L | Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.2 mg | 119 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 15 | 41 | Chem. 17[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 mg | 124 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 16 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys 16, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 96 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 17 | 41 | Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to G-Aeg | Free | Linear | L | Chem.7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16, Aib modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.2 mg | 105 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 18 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Amidation | Linear | L | Chem.11 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19- carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys20, Sar2 modification | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 88 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Parent compound 1 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 8 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 nmol/kg | 121 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 2.1 | |||
| N.A. | 2023 | Parent compound 2 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 1 nmol/kg | 104 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 1.5 | |||
| N.A. | 2023 | Parent compound 4 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 1 nmol/kg | 106 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4.2 | |||
| N.A. | 2023 | Non-converting compound 1 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Aib at position 4, Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 nmol/kg | 170 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 1 | 41 | D-Lys conjugated with [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] | Free | Linear | Mix | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 , Sar2 modification | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 20 nmol/kg | 118 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 3 | 41 | Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 nmol/kg | 119 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 9 | 41 | Chem. 19[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]acetyl] attached to Lys1 | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 20 nmol/kg | 102 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 10 | 41 | Chem. 21[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to D-Lys1 | Free | Linear | Mix | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4- carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 20 nmol/kg | 118 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for Pk Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 20 mg/kg | 27 | Cynomolgus monkeys serum protease | Sandwich ELISA | Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 28 ± 23 | Cynomolgus monkeys serum protease | Sandwich ELISA | Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 20 mg/kg | 26.5 | C2 Cynomolgus monkeys serum protease | Sandwich ELISA | C2 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 13.4 | C4 Cynomolgus monkeys serum protease | Sandwich ELISA | C4 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 54.4 | C5 Cynomolgus monkeys serum protease | Sandwich ELISA | C5 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Alb23-Fc-ABDEG | 341 | Alb23 fused at the N-termini of both Fc domains of efgartigimod | Free | Linear | L | None | Synthetic | FcRN Antagonist | Blood sample were collected for PK Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43 | 5 mg/kg | 16.9 | C6 Cynomolgus monkeys serum protease | Sandwich ELISA | C6 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 30 mg/kg | 15 | G1-1 Cynomolgus monkeys serum protease | Sandwich ELISA | G1-1 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 30 mg/kg | 9.3 | G1-2 Cynomolgus monkeys serum protease | Sandwich ELISA | G1-2 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 30 mg/kg | 4.5 | G1-3 Cynomolgus monkeys serum protease | Sandwich ELISA | G1-3 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | FcRN Antagonist | N.A. | 75 mg/kg | 13 | G2-1 Cynomolgus monkeys serum protease | Sandwich ELISA | G2-1 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | Fcrn Antagonist | N.A. | 75 mg/kg | 6.1 | G2-2 Cynomolgus monkeys serum protease | Sandwich ELISA | G2-2 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | TA-Fc-ABDEG-Alb23 | 361 | Free | Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker | Linear | L | None | Synthetic | Fcrn Antagonist | N.A. | 75 mg/kg | 12 | G2-3 Cynomolgus monkeys serum protease | Sandwich ELISA | G2-3 Cynomolgus monkeys serum | In Vivo | None | EP 2023066180 W | N.A. | |||
| N.A. | 2023 | ZTPA001 | 108 | Free | ABD (albumin Binding Domain) | Linear | L | None | Tslp Binding Z Variants | Antiinflammatory | Blood samples (0.5 mL) were collected at the following time points: Predose, At 10 And 30 Min And 1 , 6, 10, 26, 50, 72, And 96 H Postdose And At Days 6, 7, 8, 11 , 13, 15, 18, And 22 | 1.33 mg/kg | 3-4 (Terminal Half Life) | Cynomolgus monkeys serum protease | Sandwich PK-ELISA | Cynomolgus monkeys serum | In Vivo | None | EP 2023053030 W | IC50(nM) = 0.5 | |||
| N.A. | 2023 | ZTPA104 | 111 | ABD (albumin Binding Domain) | Free | Linear | L | None | Tslp Binding Z Variants | Antiinflammatory | Blood sampling time points were divided into two cohorts as follows: Cohort A (N=3 Per Test Item) Were Bled Predose, At 5 Min And 1 , 8, 72, 168, 264, 408 And 504 H Postdose; And Cohort B (N=3 Per Test Item) Were Bled Predose, At 30 Min And 3, 24, 120, 216, 336 And 456 H Postdose | 1.2 mg/kg | 36 (Terminal Half Life) | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | EP 2023053030 W | IC50(nM) = 0.03 | |||
| N.A. | 2023 | ZTPA001 | 108 | Free | ABD (albumin Binding Domain) | Linear | L | None | Tslp Binding Z Variants | Antiinflammatory | Blood sampling time points were divided into two cohorts as follows: Cohort A (N=3 Per Test Item) Were Bled Predose, At 5 Min And 1 , 8, 72, 168, 264, 408 And 504 H Postdose; And Cohort B (N=3 Per Test Item) Were Bled Predose, At 30 Min And 3, 24, 120, 216, 336 And 456 H Postdose | 1.2 mg/kg | 29 (Terminal Half Life) | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | EP 2023053030 W | IC50(nM) = 0.5 | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 0.65 ± 0.04 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | PEG Rh(27.7Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 6.59 ± 0.27 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-PEGMw | 39 | Fluorescently labelled | PEG MW(46.3 Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 6.6 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 2.7 ± 0.5 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | PEGMAopt(54.7Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 9.1 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 2.8 ± 0.7 | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 0.77 ± 0.07 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | PEG RH(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | N.A. | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | POEGMAopt(54.7Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 12.1 ± 1.0 (T1/2 Absorption) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 2.8 ± 0.7 | |||
| 36630826 | 2023 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 0.65 ± 0.04 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Free | PEGylation | Linear | L | Fluorescently labeled | Synthetic | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 6.59 ± 0.27 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-PEGMw | 39 | Free | PEGylation | Linear | L | Fluorescently labeled | Synthetic | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 6.6 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 2.7 ± 0.5 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Free | POEGMA conjugation | N.A. | L | Fluorescently labeled | Synthetic | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 9.1 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 0.77 ± 0.07 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 38092894 | 2023 | tag-free rhMFG-E8 | 387 | Cystatin S | Free | Linear | L | Glycosylation | Derived from Expi293F Human cells | antiinflammatory | Blood samples (100 μl per time point) were collected at 0, 3, 6, 9, 12 and 15 min, then every 15 min for the first 60 min till 2 hours | 50 µg | 11.55 (Distribution Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | LD50/30 (lethal dose, 50% at 30 days) falls between 14.5 Gy and 15 Gy after partial body irradiation (PBI) in mice treated with vehicle (normal saline), | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration | 260 μg/kg | 54.5 | Mouse serum protease | Modified ELISA | Mouse serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration | 260 μg/kg | 32.3 | Mouse serum protease | Modified ELISA | Mouse serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration | 260 μg/kg | 66.4 ± 33.0 | Rats serum protease | Modified ELISA | Rats serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration | 260 μg/kg | 40.9 ± 17.7 | Rats serum protease | Modified ELISA | Rats serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration | 52 μg/kg | 24.9 ± 2.2 | Dogs serum protease | Modified ELISA | Dogs serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration | 52 μg/kg | 26.6 ± 1.5 | Dogs serum protease | Modified ELISA | Dogs serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | Compound 14 | 40 | Free | Amidation | Linear | Mix | D-Ser2 substiuition, Lys14 side chain linked to C16 fatty acid via linker yE-C16 | GLP-1 analogs | Dual GLP-1/Glucagon receptor agonist | The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application | 1 mg/kg | 3.2 | C57/B16 female mice plasma protease | LC−MS/MS | C57/B16 female mice plasma | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | GLP-1 receptor : EC50 = 3.9 pM | |||
| 36997003 | 2023 | Compound 15 | 41 | Free | Terminal Lys side chain linked to C16 fatty acid via linker yE-C16 at C terminal | Linear | Mix | D-Ser2 substiuition | GLP-1 analogs | Dual GLP-1/Glucagon receptor agonist | The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application | 1 mg/kg | 2.2 | C57/B16 female mice plasma protease | LC−MS/MS | C57/B16 female mice plasma | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | GLP-1 receptor : EC50 = 5.2 pM | |||
| 36997003 | 2023 | Liraglutide | 32 | Free | Free | Linear | L | Lys20 side chain linked to C16 fatty acid via linker yE-C16 | GLP-1 analogs | Dual GLP-1/Glucagon receptor agonist | The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application | 1 mg/kg | 3.6 | C57/B16 female mice plasma protease | LC−MS/MS | C57/B16 female mice plasma | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | GLP-1 receptor : EC50 = 6.4 pM | |||
| 37242650 | 2023 | ELA | 32 | pGlu = Pyroglutamate | Free | Cyclic (C17-C22 disulfide bond) | L | None | Human derived | Endogenous Ligand of APJ | Incubated at 37°C for 2, 5 and 10 min | 1 mM | Almost completely degraded after 2 min | Rats plasma protease | HPLC-MS | Rats plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/26986036/ | None | Gαi1 EC50 (nM) = 5.3 ± 2.5 | |||
| 37329900 | 2023 | KAN-101 | N.A. | N.A. | N.A. | N.A. | N.A. | Liver-targeting glycosylation signature conjugated to a deaminated gliadin peptide | N.A. | Liver-Targeted Immune Tolerance Therapy | N.A. | 0·15 mg/kg, 0·3 mg/kg, 0·6 mg/kg, 1·2 mg/kg, 1·5 mg/kg | 3·72 to 31·72 | Human protease | N.A. | Human | In Vivo | None | None | N.A. | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 54.5 | Mouse serum protease | ELISA | Mouse serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 32.3 | Mouse serum protease | ELISA | Mouse serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 66.4 ± 33.0 | Rats serum protease | ELISA | Rats serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 260 μg/kg | 40.9 ± 17.7 | Rats serum protease | ELISA | Rats serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 52 μg/kg | 24.9 ± 2.2 | Dogs serum protease | ELISA | Dogs serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36997003 | 2023 | HM15136 | 240 | Free | HMC001 | Cyclic (E36-K40 lactam bridge in GCG analog) | L | Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker | Glucagon analog | Treatment of Congenital Hyperinsulinism | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136 | 52 μg/kg | 26.6 ± 1.5 | Dogs serum protease | ELISA | Dogs serum | In Vivo | PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/ | None | KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration | 20 μg/kg | 15.2 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 18.5 | SD rats plasma protease | LC-MS/MS | SD rats plasma dosed with BPC once a day for seven consecutive days | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration | 20 μg/kg | 7.87 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 17.1 | SD rats plasma protease | LC-MS/MS | SD rats plasma dosed with BPC once a day for seven consecutive days | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration | 500 μg/kg | 29.7 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 6 μg/kg | 5.27 ± 2.25 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 30 μg/kg | 19.6 ± 3.72 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma with repeated dose of 30 μg/kg for seven consecutive days | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 6 μg/kg | 20.0 ± 5.53 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 30 μg/kg | 25.5 ± 7.08 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 150 μg/kg | 29.3 ± 5.06 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | [3H]BPC157 | 15 | Free | Free | Linear | L | all Proline radiolabelled with [3H] | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Whole blood and plasma samples of six JVC rats were collected at 0.05, 0.167, 0.5, 1, 2, 4, 8, 24, 48, and 72 h after administration (three males and three females at each time point) for the examination of radio pharmacokinetics of total plasma | 100 µg/300 μCi/kg | 102 ± 32 | JVC rats plasma protease | Liquid scintillation counter | JVC Rats plasma | In Vivo | None | None | N.A. | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | https://pmc.ncbi.nlm.nih.gov/articles/PMC7994712/ | None | IC50(nM) = 1.7 (relative affinities of CST for the different Somatostatin receptor SSTR1) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.09 (relative affinities of CST for the different Somatostatin receptor SSTR2) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.3 (relative affinities of CST for the different Somatostatin receptor SSTR3) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.2 (relative affinities of CST for the different Somatostatin receptor SSTR4) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.3 (relative affinities of CST for the different Somatostatin receptor SSTR1) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 47.3 (relative affinities of A5 for the different Somatostatin receptor SSTR1) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 35 (relative affinities of A5 for the different Somatostatin receptor SSTR2) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 5.1 (relative affinities of A5 for the different Somatostatin receptor SSTR3) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 4.1 (relative affinities of A5 for the different Somatostatin receptor SSTR4) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 1.12 (relative affinities of A5 for the different Somatostatin receptor SSTR1) | |||
| 36557850 | 2022 | Leuprolide | 9 | pGlu = Pyroglutamate | NHEt (Ethylamine) | Linear | Mix | d-Leucine6 substituitions | Synthetic | Anticancer (Treatment of Advanced Prostate Cancer) | Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min) | 0.1 mg/kg | 38.2 ± 4.3 (Terminal Elimination Half Life) | Male SD Rats Plasma Protease | UPLC-MS/MS | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 36557850 | 2022 | LOC | 9 | Free | Leuprolide acetate with the hydroxyl groups of leuprolide acetate | Linear | Mix | Ole = oleic acid conjugation | Synthetic | Anticancer (Treatment of Advanced Prostate Cancer) | Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min) | 0.122 mg/kg | 172 ± 66 (Terminal Elimination Half Life) | Male SD Rats Plasma Protease | UPLC-MS/MS | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 36557850 | 2022 | Leuprolide | 9 | pGlu = Pyroglutamate | NHEt (Ethylamine) | Linear | Mix | d-Leucine6 substituitions | Synthetic | Anticancer (Treatment of Advanced Prostate Cancer) | Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min) | 0.1 mg/kg | 166 ± 38 | Male SD Rats Plasma Protease | UPLC-MS/MS | Male SD rats plasma after LOC peptide administration | In Vivo | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 | 12 | Free | Free | Linear | L | Cysteine was introduced at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 1.7 | Human plasma protease | Flow cytometry-based functional assay and mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 | 12 | Free | Free | Linear | L | Cysteine was introduced in the sequence of both peptides at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 0.7 | Human plasma protease | Flow cytometry-based functional assay and mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 | 12 | Free | Free | Linear | L | Cysteine was introduced at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 7 | Human plasma protease | Antibody-competition assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 | 12 | Free | Free | Linear | L | Cysteine was introduced in the sequence of both peptides at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 9 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 | 12 | Free | Free | Linear | L | Cysteine was introduced in the sequence of both peptides at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 6 | Human plasma protease | Functional stability assay | Human plasma after GuHCl + DTT treatment | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 | 12 | Free | Free | Linear | L | Cysteine was introduced at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 5 | Human plasma protease | Mass spectrometry | Human plasma after GuHCl + DTT treatment | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (C10S) | 12 | Free | Free | Linear | L | Cys10 replaced by Ser10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 4 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys10 residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 5 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (C10S) | 12 | Free | Free | Linear | L | Cys replaced by Ser | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 4 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 3 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 6 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (C10S) | 12 | Free | Free | Linear | L | Cys replaced by Ser | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 7 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 3 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (C10S) | 12 | Free | Free | Linear | L | Cys replaced by Ser | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 4 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36471433 | 2022 | [125I]sNEP-scFv8D3-scFc | 1456 | sNEP (amino acid 52–749 of NEP) recombinantly linked to a single-chain fragment constant (scFc) of mouse IgG2c antibody at N terminus using linker | ScFc then attached to the BBB transporter (scFv8D3) at C terminus using linker | Linear | L | 125I labeled | Fusion protein of sNEP-scFc-scFv8D3 | Treatment of Alzheimer's diseases | Blood samples collected from the tail vein at 1, 4, 6, 24, 48 and 72 h post-administration | 5 mg/kg | 16 | Tg-Arcswe Mice Plasma Protease | instant thin layer chromatography (iTLC) | Tg-ArcSwe mice plasma | In Vivo | None | None | N.A. | |||
| 36471433 | 2022 | [125I]muNEP-scFv8D3-scFc | 1456 | sNEP (amino acid 52–749 of NEP) recombinantly linked to a single-chain fragment constant (scFc) of mouse IgG2c antibody at N terminus using linker | ScFc then attached to the BBB transporter (scFv8D3) at C terminus using linker | Linear | L | 125I labeled | Fusion protein of sNEP-scFc-scFv8D3 | Treatment of Alzheimer's diseases | Blood samples collected from the tail vein at 1, 4, 6, 24, 48 and 72 h post-administration | 2.5 mg/kg | 18 | Tg-Arcswe Mice Plasma Protease | instant thin layer chromatography (iTLC) | Tg-ArcSwe mice plasma | In Vivo | None | None | N.A. | |||
| 36443381 | 2022 | SA10SC-RLX | 25 | Acetylation | Amidation | Linear | L | Attachment of a lipid moiety (C18-γ-Glu-PEG2) at K25 position, Aib, Nle,acetylation of Lys10 | Synthetic | Treatment for Chronic Fibrotic and Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48 and 72 h (IV route) and 0.25, 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h (SC route) | 1 mg/kg | 4 (Terminal Half Life) | Rats plasma protease | LC-HRMS | Rats plasma | In Vivo | None | None | EC50 (nM) = 0.8 for EA.hy926_hRXFP1 | |||
| 36443381 | 2022 | SA10SC-RLX | 25 | Acetylation | Amidation | Linear | L | Attachment of a lipid moiety (C18-γ-Glu-PEG2) at K34 position, Aib, Nle | Synthetic | Treatment for Chronic Fibrotic and Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 2, 4, 6, 8, 24, 48, 72, 96 and 168 h (IV route) and 0.25, 0.5, 2, 4, 6, 8, 24, 48, 72, 96 and 168 h (SC route) | 1 mg/kg | 7 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50 (nM) = 0.8 for EA.hy926_hRXFP1 | |||
| 36443291 | 2022 | Entry 1 (aka P5779) | 4 | Free | Amidation | Linear | L | None | Synthetic | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.0 ± 0.1 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 68.5 nM | |||
| 36443291 | 2022 | Entry 2 (Azapeptide 51) | 4 | Aza-Phe at postion 1 | Amidation, Aza-glutamic acid (azaE4) modification at position 4 (E4) | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | >120 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 90 nM | |||
| 36443291 | 2022 | Entry 3 (Azapeptide 52) | 4 | Aza-Phe at postion 1 | Amidation | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | >120 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 249 nM | |||
| 36443291 | 2022 | Entry 4 (Azapeptide 53) | 4 | Free | Aza-glutamic acid (azaE4) modification at position 4 (E4) | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.6 ± 0.11 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 396.8 nM | |||
| 36443291 | 2022 | Entry 5 (Azapeptide 54) | 4 | Aza-Phe at postion 1 | Amidation | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | >120 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 127.4 nM | |||
| 36443291 | 2022 | Entry 6 (Azapeptide 55) | 4 | Aza-Phe at postion 1 | Amidation, Q amino acid subtituition at place of E at C terminal | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 24.4 ± 1.6 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 159.3 nM | |||
| 36443291 | 2022 | Entry 7 (Azapeptide 56) | 4 | Aza-Phe at postion 1 | Amidation, Q amino acid subtituition at place of E at C terminal | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | >120 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 348.7 nM | |||
| 36443291 | 2022 | Entry 8 (Azapeptide 57) | 4 | Aza-Phe at postion 1 | Amidation, Aza-glutamine (azaQ4) | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | >120 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 83 nM | |||
| 36443291 | 2022 | Entry 9 (Azapeptide 58) | 4 | Free | Amidation, Aza-glutamine (azaQ4) | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.9 ± 0.20 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 422.9 nM | |||
| 36443291 | 2022 | Entry 1 (Bradykinin) | 9 | Free | Free | Linear | L | None | Derived from kininogen | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 5.29 ± 0.5 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 44.4 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 2 (azaR1-BK) | 9 | Modified at position 1 with an aza-amino acid (aza-arginine) | Free | Linear | L | None | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.46 ± 0.05 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 3(azaP2-BK) | 9 | Free | Free | Linear | L | Modified at position 2 with an aza-amino acid (aza-proline) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 5.40 ± 1.1 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 61.1 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 4 (azaP3-BK) | 9 | Free | Free | Linear | L | Modified at position 3 with an aza-amino acid (aza-proline) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.63 ± 0.25 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 5 (azaG4-BK) | 9 | Free | Free | Linear | L | Modified at position 4 with an aza-amino acid (aza-glycine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 4.33 ± 1.3 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 6 (azaF5-BK) | 9 | Free | Free | Linear | L | Modified at position 5 with an aza-amino acid (aza-phenylalanine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 14.7 ± 1.6 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 7 (azaP7-BK) | 9 | Free | Free | Linear | L | Modified at position 7 with an aza-amino acid (aza-proline) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.38 ± 0.03 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 8 (azaF8-BK) | 9 | Free | Free | Linear | L | Modified at position 8 with an aza-amino acid (aza-phenylalanine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 39.3 ± 2.5 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 99.6 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 9 (azaR9-BK) | 9 | Free | Free | Linear | L | Modified at position 9 with an aza-amino acid (aza-arginine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 42.6 ± 0.8 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 10 ([azaP2, azaF8]-BK) | 9 | Free | Free | Linear | L | Modified at both positions 2 and 8 with aza-amino acids (aza-proline and aza-phenylalanine, respectively) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 29.2 ± 3.8 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 80.6 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 11 ([azaF5, azaF8]-BK) | 9 | Free | Free | Linear | L | Modified at both positions 5 and 8 with aza-amino acids (aza-phenylalanine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 105.8 ± 1.8 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | 37 °C | 0.3 nmol | 10.2 ± 0.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | PDB id: 5VAI | None | BGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | 37 °C | 6 nmol | 55.7 ± 12.1 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | PDB id: 5VAI | None | BGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glc-GLP-1-1 | 31 | Free | Free | Linear | L | Glucosylation at Asn15 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 30.2 ± 2.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-1 | 31 | Free | Free | Linear | L | Glucosylation at Asn15 | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 94.1 ± 7.6 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-3 | 31 | Free | Free | Linear | L | Glucosylation at Asn26 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 46.1 ± 3.5 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-3 | 31 | Free | Free | Linear | L | Glucosylation at Asn26 | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 138.8 ± 14.5 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-5 | 31 | Free | Free | Linear | L | Glucosylation at Asn34 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 32.5 ± 1.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-5 | 31 | Free | Free | Linear | L | Glucosylation at Asn34 | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 113.3 ± 11.8 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn15 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 49.1 ± 5.7 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 24.44 ± 2.37 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn15 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 355.5 ± 9.3 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 24.44 ± 2.37 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 145.7 ± 4.3 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 736.6 ± 12.3 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 185.3 ± 1.1 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 738.6 ± 9.7 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn26 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 374.7 ± 1.8 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 25.71 ± 3.19 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn26(G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 1393.1 ± 8.9 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 25.71 ± 3.19 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn34 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 182.0 ± 0.1 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 14.50 ± 1.62 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn34 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 390.4 ± 13.5 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 14.50 ± 1.62 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 245.3 ± 1.3 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 777.0 ± 10.2 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability) | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 228 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 3.8 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M1 | 35 | Free | Two lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 17 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.068 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M2 | 34 | Free | 1 lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 231 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 254 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal , Amidation | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 2.8 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M1 | 35 | Free | Two lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 37.7 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.068 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M2 | 34 | Free | 1 lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 255 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 88.3 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 10.4 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal , Amidation | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 11.7 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M1 | 35 | Free | Two lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 1.2 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.068 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M2 | 34 | Free | 1 lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 2.6 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36232550 | 2022 | ASK2131 | 9 | Free | Free | Cyclic (C1-C6 Disulfide Bond) | L | Native oxytocin peptide was modified with a substitution of the Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group and with a substitution of Gly for the Pro7 | OXT analogs | Antiobesity | Serial blood samples (200 µL per time point) were obtained via tail nick using K3EDTA microvettes prior to and 1, 2, 4, 6, 12, and 24-h post-drug administration | 300 nmol/kg | 2.3 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50 = 1.1 nM (ASK2131 profile against OXTR ) | |||
| 36232550 | 2022 | ASK2131 | 9 | Free | Free | Cyclic (C1-C6 Disulfide Bond) | L | Native oxytocin peptide was modified with a substitution of the Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group and with a substitution of Gly for the Pro7 | OXT analogs | Antiobesity | Serial blood samples (200 µL per time point) were obtained via tail nick using K3EDTA microvettes prior to and 1, 2, 4, 6, 12, and 24-h post-drug administration | 300 nmol/kg | 2.3 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | hV1aR, EC50 (nM) > 1000 | |||
| 36232550 | 2022 | ASK2131 | 9 | Free | Free | Cyclic (C1-C6 Disulfide Bond) | L | Native oxytocin peptide was modified with a substitution of the Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group and with a substitution of Gly for the Pro7 | OXT analogs | Antiobesity | Serial blood samples (200 µL per time point) were obtained via tail nick using K3EDTA microvettes prior to and 1, 2, 4, 6, 12, and 24-h post-drug administration | 300 nmol/kg | 2.3 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | hV2R, EC50 (nM) = 0.36 | |||
| 36142749 | 2022 | PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | opioid–neurotensin hybrid peptide | Analgesic | 37°C for 24 h | 50 μg/mL | 204.4 | N.A. | LC-MS | 1M HCl | In Vitro | None | None | Emax = 149.17% ± 2.9 for PK20 (intrinsic activity of the receptor) | |||
| 36142749 | 2022 | PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | opioid–neurotensin hybrid peptide | Analgesic | 37°C for 24 h | 50 μg/mL | 11.36 | N.A. | LC-MS | 1M NaOH | In Vitro | None | None | EC50 = 79 nM (potency at mu opioid receptor) | |||
| 36142749 | 2022 | [Ile9]PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | PK20 derivative | Analgesic | 37°C for 24 h | 50 μg/mL | 117.7 | N.A. | LC-MS | 1M HCl | In Vitro | None | None | Emax = 151.2% ± 74.5 for [Ile9]PK20 (intrinsic activity of the receptor) | |||
| 36142749 | 2022 | [Ile9]PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | PK20 derivative | Analgesic | 37°C for 24 h | 50 μg/mL | 4.69 | N.A. | LC-MS | 1M NaOH | In Vitro | None | None | EC50 = 1244 nM (potency at mu opioid receptor) | |||
| 36135098 | 2022 | GNRs-AAP1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 0.29 (T1/2 a) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 37.81 (T1/2 b ) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 0.18 (T1/2 a) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 7.7 (T1/2 b) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-2-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 0.2 (T1/2 a) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-2-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 5 (T1/2 Β ) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | N.A. | 1 mg/kg | 1 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | N.A. | 1 mg/kg | 0.9 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | N.A. | 1.25 mg/kg | 1.7 | NHP plasma protease | LC-MS/MS | NHP plasma | In Vivo | None | None | KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | >57.8 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | KD(nM) = 2.5±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in human) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | >57.8 | NHP plasma protease | LC-MS/MS | NHP plasma | In Vitro | None | None | KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 60.7 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 2.3 - 4.4 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 26.1 | Human blood Protease | LC-MS/MS | Human blood sample | In Vitro | None | None | KD(nM) = 2.5±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in human) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 28.3 | NHP blood protease | LC-MS/MS | NHP blood sample | In Vitro | None | None | KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 8.5 | Rats blood protease | LC-MS/MS | Rats blood sample | In Vitro | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 5 | Mouse blood protease | LC-MS/MS | Mouse blood sample | In Vitro | None | None | KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse) | |||
| 36101452 | 2022 | IgG1 S-AM (6-52) | 47 | IgG1 Fc linked with hAM using linker (GGGGS)3 | Amidation | Cyclic (C16-C21 Disulfide Bond In Ham) | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 2.11 | Wistar rats plasma protease | ELISA (measure mAM) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | IgG4 S-AM (6-52) | 47 | IgG4 Fc linked with hAM using linker (GGGGS)3 | Amidation | Linear | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 2.37 | Wistar rats plasma protease | ELISA (measure mAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | IgG1 S-AM (6-52) | 47 | IgG1 Fc linked with hAM using linker (GGGGS)3 | Amidation | Cyclic (C16-C21 Disulfide Bond In Ham) | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 2.885 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | IgG4 S-AM (6-52) | 47 | IgG4 Fc linked with hAM using linker (GGGGS)3 | Amidation | Linear | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 3.23 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | AM | 52 | Free | Amidation | Cyclic (C16-C21 Disulfide Bond) | L | None | Isolated from Human pheochromocytoma | Vasodilator and Cardiovascular Protection | Blood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration | 50 nmol/kg | 32.3 | Wistar rats plasma protease | ELISA (measure mAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | AM | 52 | Free | Amidation | Cyclic (C16-C21 Disulfide Bond) | L | None | Isolated from Human pheochromocytoma | Vasodilator and Cardiovascular Protection | Blood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration | 50 nmol/kg | 27.5 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36075899 | 2022 | S-20-1 | N.A. | N.A. | N.A. | Cyclic | L | Modified by adding negative charge | Synthetic | Antiviral (Against Infection By Sars-Cov-2 ) | Blood samples were collected at 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h | 50 mg/kg | 14.53 (Terminal Elimination Half Life) | C57Bl/6 mice plasma protease | LC-MS/MS | C57BL/6 mice plasma | In Vivo | None | None | IC50 (μM) = 0.8 in HUH 7 cells | |||
| 36075899 | 2022 | S-20-1 | N.A. | N.A. | N.A. | Cyclic | L | Modified by adding negative charge | Synthetic | Antiviral (Against Infection By Sars-Cov-2 ) | Blood samples were collected at 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h | 50 mg/kg | 24.29 (Terminal Elimination Half Life) | C57Bl/6 mice plasma protease | LC-MS/MS | C57BL/6 mice plasma | In Vivo | None | None | IC50 (μM) = 0.8 in HUH 7 cells | |||
| 36047255 | 2022 | MTP/RGD-CAL/TAN NS | 4 for MTP, 3 for cRGD | Free | MTP/RGD comodified with CAL/TAN NS | Linear | L(cRGD), Mix(MTP) | Dmt: 2',6'-dimethyltyrosine | Synthetic | Treatment of Acute Myocardial Infarction (Ami) | Blood samples were obtained at determined times until 72 h after injection and 15 μL of heparin (1000 U/mL) was added to each sample | 10 mg/kg | 8.22 | AMI rats plasma protease | N.A. | AMI rats plasma | In Vivo | None | None | Blank MTP/RGD NS and RGD-PEG-DSPE groups showed over 85% of cell viability. In contrast, drugs contained formulations exhibited cytotoxicity to some extent | |||
| 36047255 | 2022 | MTP-CAL/TAN NS | 5 | Free | MTP/RGD comodified with CAL/TAN NS (PEG-DSPE) | Linear | Mix | Dmt: 2',6'-dimethyltyrosine at position 3, D-Arg2 modification | Synthetic | Treatment of Acute Myocardial Infarction (Ami) | Blood samples were obtained at determined times until 72 h after injection and 15 μL of heparin (1000 U/mL) was added to each sample | 10 mg/kg | 4.59 | AMI rats plasma protease | N.A. | AMI rats plasma | In Vivo | None | None | Blank MTP/RGD NS and RGD-PEG-DSPE groups showed over 85% of cell viability. In contrast, drugs contained formulations exhibited cytotoxicity to some extent. | |||
| 36034808 | 2022 | uPAR | 335 | Free | Free | Linear | L | None | Derived from PLAUR gene | Plays role in thrombosis | N.A. | N.A. | 209.6 ± 0.2 | BEAS-2B cells lysate protease | Densitometry analysis using NIH Image J | BEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + Cycloheximide | In Vivo | None | None | N.A. | |||
| 36034808 | 2022 | uPAR | 335 | Free | Free | Linear | L | None | Derived from PLAUR gene | Plays role in thrombosis | N.A. | N.A. | 48.2 ± 2.3 | BEAS-2B cells lysate protease | Densitometry analysis using NIH Image J | BEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + Cycloheximide | In Vivo | None | None | N.A. | |||
| 35999612 | 2022 | cRGD-Exo/TP | 3 | DSPE-PEG | Free | Cyclic (RGD) | L | DiR labeled | Synthetic | Targeted delivery of triptolide against malignant melanoma | Scanned at interval times (1, 2, 4, 6, 12, and 24 h) | N.A. | 27.14 ± 2.55 | Mice plasma protease | IVIS at 750/780 nm | BALB/c nude mice plasma | In Vivo | None | None | Tumor inhibition rate of 65.73 ± 3.29% in the cRGD-Exo/TP | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 20 nmol/kg | 10.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18059 pmol/kg | 12.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18058 pmol/kg | 10.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17872 pmol/kg | 18.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18052 pmol/kg | 12.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17838 pmol/kg | 8.5 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17881 pmol/kg | 8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17833 pmol/kg | 8.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17941 pmol/kg | 7.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18000 pmol/kg | 7.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17890 pmol/kg | 8.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18117 pmol/kg | 8.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35971165 | 2022 | Au‐AR pep‐PROTAC | 33 | Free | Free | Linear | L | None | Synthetic | Anticancer (Prostate Cancer Therapy) | N.A. | N.A. | 26.3 | Mouse serum protease | ICP‐MS | mouse serum | In Vivo | None | None | N.A. | |||
| 35971165 | 2022 | Au‐AR pep‐PROTAC | 33 | Free | Free | Linear | L | None | Synthetic | Anticancer (Prostate Cancer Therapy) | N.A. | N.A. | 25.1 | PBS containing 10% serum protease | HPLC | PBS containing 10% serum | In Vitro | None | None | IC50 of Au‐AR pep‐PROTAC on AML 12 cells is 2.41 µM | |||
| 35971165 | 2022 | AR pep‐PROTAC | 33 | Free | Free | Linear | L | None | Synthetic | Anticancer (Prostate Cancer Therapy) | N.A. | N.A. | 1.9 | PBS containing 10% serum protease | HPLC | PBS containing 10% serum | In Vitro | None | None | IC50 of Au‐AR pep‐PROTAC on AML 12 cells is 2.41 µM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | Blood samples were collected before RA15127343 administration (baseline) and 1–4 times per day until study end. | 10 nmol/kg | 47 | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | Blood samples were collected before RA15127343 administration (baseline) and 1–4 times per day until study end. | 10,30,45,60 nmol/kg | 48 - 59 | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | N.A. | 200 nmol/kg | 11 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | N.A. | 200, 400 nmol/kg | 21 - 22 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35890224 | 2022 | 177Lu-Palm-3PRGD2 | 2 | Lys1 linked with (palmitoyl-Glu-OH) | Glu3 linked with (PEG4-c(RGDfK))2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between | Synthetic | Antitumor | N.A. | 0.74 MBq | 4.49 (T1/2a) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | Synthetic | Antitumor | N.A. | 0.74 MBq | 1.94 (T1/2a) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-Palm-3PRGD2 | 2 | Lys1 linked with (palmitoyl-Glu-OH) | Glu3 linked with (PEG4-c(RGDfK))2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between | Synthetic | Antitumor | N.A. | 0.74 MBq | 73.42 (T1/2Β) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | Synthetic | Antitumor | N.A. | 0.74 MBq | 11.81 (T1/2Β) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-Palm-3PRGD2 | 2 | Lys1 linked with (palmitoyl-Glu-OH) | Glu3 linked with (PEG4-c(RGDfK))2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between | Synthetic | Antitumor | N.A. | 0.74 MBq | 63.71 (Slow) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | Synthetic | Antitumor | N.A. | 0.74 MBq | 14.54 (Slow) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-Palm-3PRGD2 | 2 | Lys1 linked with (palmitoyl-Glu-OH) | Glu3 linked with (PEG4-c(RGDfK))2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between | synthetic | Antitumor | N.A. | 0.74 MBq | 2.08 (Fast) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | synthetic | Antitumor | N.A. | 0.74 MBq | 1.06 (Fast) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35858423 | 2022 | 4A | 38 | 3A coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2CHSO2-, N3-linker N-hydroxysuccinymidocarbonates containing isopropyl sulfone (1A) and N,N-dimethyl-sulfonamide (1B) modulators | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600 and 672 h on a staggered schedule from 12 mice to give 4 replicates at each time-point | 20 nmol | 40 (T1/2,a -Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | QWk 50 nmol of 4A caused significantly increased growth, with mice becoming about 25% longer than the vehicle control over the study period | |||
| 35858423 | 2022 | 4B | 38 | 3B coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2CHSO2-, N3-linker N-hydroxysuccinymidocarbonates containing N,N-dimethyl-sulfonamide (1B) modulators | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 24, 96, 168, 240, 336, 408, 504, 576, 672, 840, 1008, 1176, 1344, and 1512 h from 8 mice on a staggered schedule to give 4 replicates at each time-point | 700 nmol | 60 ( T1/2,a - Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | Single dose of 85 nmol of 4B showed similar growth stimulation as QD administration of [Gln6,14]CNP-38 for 3 weeks, but growth plateaued afterward | |||
| 35858423 | 2022 | 4A | 38 | 3A coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2CHSO2- | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600 and 672 h on a staggered schedule from 12 mice to give 4 replicates at each time-point | 20 nmol | 212 (T1/2,b-Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | QWk 50 nmol of 4A caused significantly increased growth, with mice becoming about 25% longer than the vehicle control over the study period | |||
| 35858423 | 2022 | 4B | 38 | 3B coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2NSO2- | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 24, 96, 168, 240, 336, 408, 504, 576, 672, 840, 1008, 1176, 1344, and 1512 h from 8 mice on a staggered schedule to give 4 replicates at each time-point | 700 nmol | 610 ( T1/2,b-Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | Single dose of 85 nmol of 4B showed similar growth stimulation as QD administration of [Gln6,14]CNP-38 for 3 weeks, but growth plateaued afterward | |||
| 35850571 | 2022 | dTBP2 | 7 | Free | Free | Linear | L | None | dTCTP-binding peptide-2 | Antiinflammatory | Blood samples were collected from the orbital sinus at 0.083, 0.25, 0.5, 1, 2, 4, and 8 h after dosing with dTBP2 or PEG-dTBP2 | 10 mg/kg | 1.01 ± 0.25 | ICR male mice orbital sinus plasma protease | LC-MS/MS | ICR Male mice orbital sinus plasma | In Vivo | None | None | dTBP2 results in 30% inhibition of inflammatory cell infiltration in BALF compared to the OVA-challenged group | |||
| 35850571 | 2022 | PEG-dTBP2 | 7 | PEGylation (mPEG) | Free | Linear | L | None | dTCTP-binding peptide-2 | Antiinflammatory | Blood samples were collected from the orbital sinus at 0.083, 0.25, 0.5, 1, 2, 4, and 8 h after dosing with dTBP2 or PEG-dTBP2 | 10 mg/kg | 2.57 ± 1.11 | ICR male mice orbital sinus plasma protease | LC-MS/MS | ICR Male mice orbital sinus plasma | In Vivo | None | None | PEG-dTBP2 results in 45% inhibition, indicating that PEGylation enhances the anti-inflammatory effects of dTBP2 | |||
| 35849214 | 2022 | HSA | 585 | Free | Free | Cyclic (17 Disulfide Bond) | L | None | Human derived | Carrier Protein | 30 minutes | 3 mL/kg of 20% albumin | 8 | Human intravascular sample protease | N.A. | Human intravascular sample | In Vivo | None | None | N.A. | |||
| 35849214 | 2022 | HSA | 585 | Free | Free | Cyclic (17 Disulfide Bond) | L | None | Human derived | Carrier Protein | 120 minutes | 3 mL/kg of 20% albumin | 6.3 | Human intravascular sample protease | N.A. | Human intravascular sample | In Vivo | None | None | N.A. | |||
| 35840338 | 2022 | BIF | 296 | Single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | Interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 3 nmol/kg | 128 ± 10 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Receptor Phosphorylation EC50, nM = 4241 (Functional activity of BIF as determined by phosphorylation of hIR-A expressed in 293 cells) | |||
| 35840338 | 2022 | BIF | 296 | Single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | Interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 10 nmol/kg | 104 ± 4 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Receptor Phosphorylation EC50, nM = 391 (Functional activity of BIF as determined by phosphorylation of hIR-B expressed in 293 cells) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Receptor Phosphorylation EC50, nM > 10,000 (Functional activity of BIF as determined by phosphorylation of hIGF-1R expressed in 293 cells) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Lipogenesis in 3T3-L1 Adipocytes, EC50 nM = 19 (Functional activity of BIF as assessed by lipogenesis and cellular proliferation) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Proliferation in Saos-2 Cells,EC50 nM = 134 (Functional activity of BIF as assessed by cellular proliferation) | |||
| 35840338 | 2022 | BIF | 296 | single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1) | interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2 | Linear | L | None | Fc-fusion protein | Antidiabetes | Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose | 30 nmol/kg | 120 ± 21 | Streptozotocin STZ-treated diabetic SD rats blood protease | Insulin receptor ELISA | Streptozotocin STZ-treated diabetic SD rats blood sample | In Vivo | None | None | Proliferation in H4IIE Cells,EC50 nM = 20 (Functional activity of BIF as assessed by cellular proliferation) | |||
| 35807500 | 2022 | TIPP | 5 | Free | Free | Linear | L | None | From calf thymus extracts | Treatment of Asthma | At 0.5, 1, 2, 5, 10, 15, 20, and 40 min post administration (eight mice at each time points), blood samples were taken from an inner canthus | 50 mg/kg | 5.99 ± 1.82 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | TIPP inhibits degranulation and inflammation in RBL-2H3 cells and pretreatment with 200 microgram/mL of TIPP for 20 minutes reduces the level of biomarkers of allergic response and inflammation i.e β-hexosaminidase, Histamine, IL-4 | |||
| 35779189 | 2022 | NX210 | 12 | Free | Free | Linear | L | None | Derived from the subcommissural organ (SCO)-spondin | Treatment of Neurodegenerative Diseases | Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion | 2.5 mg/kg | 13.3 | Human plasma protease | HPLC–MS/MS | Human plasma | In Vivo | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3965545/ | None | N.A. | |||
| 35779189 | 2022 | NX210 | 12 | Free | Free | Linear | L | None | Derived from the subcommissural organ (SCO)-spondin | Treatment of Neurodegenerative Diseases | Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion | 5 mg/kg | 6.19 | Human plasma protease | HPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 35779189 | 2022 | NX210 | 12 | Free | Free | Linear | L | None | Derived from the subcommissural organ (SCO)-spondin | Treatment of Neurodegenerative Diseases | Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion | 10 mg/kg | 20 | Human plasma protease | HPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 35772783 | 2022 | DR7dA | 8 | Free | Amidation | Linear | Mix | Replacing the isoleucine (Ile7) residue with D-alanine7 (D-Ala) | DR8 analog | Ameliorated Tumor Growth Factor (Tgf)-B1-Induced Fibrogenesis And Bleomycin-Induced Pf | An aliquot of 40 ml was taken at 0, 15, 30, 60, 120 and 240 min | 10 mM | 201.08 ± 58.86 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | DR7dA showed no cytotoxic effects in A549 and NIH3T3 cells even at high concentrations (up to 160 μM) | |||
| 35772783 | 2022 | DR8 | 8 | Free | Amidation | Linear | L | None | Derived from rapeseed protein | Ameliorated Tumor Growth Factor (Tgf)-B1-Induced Fibrogenesis And Bleomycin-Induced Pf | An aliquot of 40 ml was taken at 0, 15, 30, 60, 120 and 240 min | 10 mM | 70.19 ± 6.83 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | The effective concentration of DR8 was higher than that of DR7dA in both cell lines, indicating that DR7dA is more potent in inhibiting fibrosis | |||
| 35710141 | 2022 | mGIPAnt‐1 | 37 | Free | Free | Linear | L | C16-diacid acylation at Lysine16 | GIP analogue | Antiobesity | Retro‐orbital blood samples (50 μl) were taken using EDTA coated glass capillaries at (1) t = 0, 0.5, 1, 1.5, 2 and 2.5 h, (2) t = 2.5, 3, 4, 6, 8 and 22 h, or (3) t = 22, 24, 26, 28, 30 and 32 h and immediately | 300 nmol/kg | 7.2 | Mouse Retro-Orbital Blood Plasma Protease | RIA | Mouse retro-orbital blood plasma | In Vivo | None | None | mGIPAnt‐1 inhibited the mouse GIP receptor with IC50 of 269 nM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.04 mmol/kg | 0.3 (Elimination Half Life) | Male SD rats plasma protease | ICP-MS | Male SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.04 mmol/kg | 0.28 (Elimination Half Life) | Female SD rats plasma protease | ICP-MS | Female SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.04 mmol/kg | 0.57(Elimination Half Life) | (P) SD rats plasma protease | ICP-MS | (P) SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.1 mmol/kg | 0.31 (Elimination Half Life) | Male SD rats plasma protease | ICP-MS | Male SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.1 mmol/kg | 0.32 (Elimination Half Life) | Female SD rats plasma protease | ICP-MS | Female SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.1 mmol/kg | 0.65 (Elimination Half Life) | (P) SD rats plasma protease | ICP-MS | (P) SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.2 mmol/kg | 0.3 (Elimination Half Life) | Male SD rats plasma protease | ICP-MS | Male SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.2 mmol/kg | 0.32 (Elimination Half Life) | Female SD rats plasma protease | ICP-MS | Female SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.2 mmol/kg | 0.22 (Elimination Half Life) | (P) SD rats plasma protease | ICP-MS | (P) SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.04 mmol/kg | 0.76 (Elimination Half Life) | Male dogs plasma protease | ICP-MS | Male dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.04 mmol/kg | 0.74 (Elimination Half Life) | Female dogs plasma protease | ICP-MS | Female dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.04 mmol/kg | 0.8 (Elimination Half Life) | (P) dogs plasma protease | ICP-MS | (P) dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.1 mmol/kg | 0.7 (Elimination Half Life) | Male dogs plasma protease | ICP-MS | Male dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.1 mmol/kg | 0.67 (Elimination Half Life) | Female dogs plasma protease | ICP-MS | Female dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.1 mmol/kg | 0.33 (Elimination Half Life) | (P) dogs plasma protease | ICP-MS | (P) dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.2 mmol/kg | 0.69 (Elimination Half Life) | Male dogs plasma protease | ICP-MS | Male dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.2 mmol/kg | 0.63 (Elimination Half Life) | Female dogs plasma protease | ICP-MS | Female dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.2 mmol/kg | 0.048 (Elimination Half Life) | (P) dogs plasma protease | ICP-MS | (P) dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35688476 | 2022 | PEG-hUCN1 | 40 | Free | Amidation | Linear | L | Insertion of a cysteine residue at position 31 for pegylation PEG20 acetamide | Human UCN1 derivative | Treating Autoimmune disease | N.A. | 0.3 mg/kg | 13 | C57Bl/6J mice plasma protease | Laser capture/mass spectrometry | C57BL/6J mice plasma | In Vivo | None | None | At the CRHR1 receptor, the PEG-hUCN1 peptide was less potent than native CRH or UCN1 peptides with EC50 values of 47, 15, and 10 nM, respectively | |||
| 35688476 | 2022 | PEG-hUCN1 | 40 | Free | Amidation | Linear | L | Insertion of a cysteine residue at position 31 for pegylation | Human UCN1 derivative | Treating Autoimmune disease | N.A. | 1 mg/kg | 17 | C57Bl/6J mice plasma protease | Laser capture/mass spectrometry | C57BL/6J mice plasma | In Vivo | None | None | At the CRHR2 receptor, the PEG-hUCN1 peptide was also less potent than UCN2 or UCN1 peptides with EC50 values of 80, 10, and 6.6 nM, respectively | |||
| 35677307 | 2022 | rhG-CSF | 175 | Free | Free | Linear | L | None | Recombinant human methionyl-granulocyte colonystimulating factor | N.A. | Sampling time - 0, 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h | 1.0 mg/kg | 2.74 ± 0.33 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35677307 | 2022 | PEG10k-rhG-CSF | 175 | Free | Free | Linear | L | PEG10K-MAL fatty chain-modification of rhG-CSF at Cys18 position | rhG-CSF derivative | N.A. | sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168h | 1.0 mg/kg | 13.05 ± 0.45 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35677307 | 2022 | C15-rhG-CSF | 175 | Free | Free | Linear | L | C15-MAL fatty chain-modification of rhG-CSF at Cys18 position | rhG-CSF derivative | N.A. | sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 h | 1.0 mg/kg | 5.72 ± 0.43 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 124 | Human Plasma Protease | LC-MS | Human plasma with Normal hepatic function | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 131 | Human Plasma Protease | LC-MS | Human plasma with Mild hepatic impairment | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 116 | Human Plasma Protease | LC-MS | Human plasma with Moderate hepatic impairment | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 122 | Human Plasma Protease | LC-MS | Human plasma with Severe hepatic impairment | In Vivo | None | None | N.A. | |||
| 35659720 | 2022 | DTX-P7 | 7 | DTX | Free | Linear | L | None | Docetaxel (DTX) and heptapeptide (P7) Fusion protein | Anticancer (Treatment Of Non-Small Cell Lung Cancer) | 1, 2, 4, 12, 24, 48 and 72 h after injection, the mice were anesthetized, and approximately 0.5 ml of blood was collected | 60 mg/kg | Longer Half Life | BALB/c mice plasma protease | HPLC | BALB/c mice bearing A549 tumors plasma | In Vivo | None | None | IC50 = 11.4 nM for DTX-P7 in A549 cells | |||
| 35659720 | 2022 | DTX-P7 | 7 | DTX | Free | Linear | L | None | Docetaxel (DTX) and heptapeptide (P7) Fusion protein | Anticancer (Treatment Of Non-Small Cell Lung Cancer) | 1, 2, 4, 12, 24, 48 and 72 h after injection, the mice were anesthetized, and approximately 0.5 ml of blood was collected | 60 mg/kg | Longer Half Life | BALB/c mice plasma protease | HPLC | BALB/c mice bearing A549 tumors plasma | In Vivo | None | None | IC50 = 0.62 nM for DTX-P7 in H1975 cells | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 4.4 ± 0.3 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35653695 | 2022 | KLK7 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 6.2 ± 0.9 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK7)(nM) = 32, Kd(albumin)(nM) = 164 (for KLK7(1)-tag) | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 5.1 ± 0.7 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 5.8 ± 0.4 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 15.3 μg/kg | 0.498 ± 0.0100 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 5 μg/kg | 3.33 ± 1.57 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 20 μg/kg | 2.83 ± 1.42 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 60 μg/kg | 2.47 ± 0.571 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | 1 day | 20 μg/kg | 3.07 ± 1.28 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | 7 days | 20 μg/kg | 1.94 ± 0.305 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35582852 | 2022 | CP | 8 | Free | PNAM37 linked through NH2 group | Cyclic(N-C terminal bond) | Mix | D-leucine at position 1 and 3 | Synthetic | Drug delivery vectors | Blood samples (0.2 mL) were taken prior to dose administration and at 1, 5, 10, 20, 30, 60, 120, 180, 240, 360, 480, and 1440 min after dose administratio | 1 μCi | 14.6 ± 2.9 (Elimination Half Life) | Rats plasma protease | Liquid scintillation counter | Rats plasma | In Vivo | None | None | For concentrations of 1 mg/mL CP , cell viabilities drop to about 75% for the 4T1 cell line | |||
| 35458385 | 2022 | FL-EK1 | 162 | Flexible 35-mer linker (L35) connects the FN3 domain to the EK1 peptide at N terminus | Free | Linear | L | None | EK1 and 10th FN3 unit conjugate | Pan-cov fusion inhibitor | Serum samples were collected before (0 h) and after injection of EK1 (0.5 h, 1 h, 3 h, 7 h, and 12 h) or FL-EK1 (0.5 h, 1 h, 3 h, 7 h, 24 h, 48 h, 72 h, and 96 h) | 40 mg/kg | 30.0 ± 12.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | IC50(nM) = 114.5 ± 33.4 against B.1.1.7 (Alpha), IC50(nM) = 201.2 ± 16.8 against B.1.351 (Beta), IC50(nM) = 373.1 ± 16.9 against P.1 (Gamma), IC50(nM) = 133.0 ± 16.5 against B.1.617.2 (Delta), IC50(nM) = 179.2 ± 38.3 against B.1.525 (Eta), IC50(nM) = 230.9 ± 49.3 against B.1.617.1 (Kappa), IC50(nM) = 88.5 ± 58.2 against C.37 (Lambda), IC50(nM) = 297.5 ± 188.2 against B.1.1.529 (Omicron) | |||
| 35458385 | 2022 | EK1 | 36 | Free | Free | Linear | L | None | Expression in E. coli | Pan-cov fusion inhibitor | Serum samples were collected before (0 h) and after injection of EK1 (0.5 h, 1 h, 3 h, 7 h, and 12 h) or FL-EK1 (0.5 h, 1 h, 3 h, 7 h, 24 h, 48 h, 72 h, and 96 h) | 8.25 mg/kg | 1.8 ± 1.0 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | IC50(nM) = 69.0 ± 20.8 against B.1.1.7 (Alpha), IC50(nM) = 109.9 ± 25.3 against B.1.351 (Beta), IC50(nM) = 191.3 ± 17.0 against P.1 (Gamma), IC50(nM) = 190.6 ± 29.0 against B.1.617.2 (Delta), IC50(nM) = 135.6 ± 11.2 against B.1.525 (Eta), IC50(nM) = 107.1 ± 7.3 against B.1.617.1 (Kappa), IC50(nM) = 68.7 ± 25.4 against C.37 (Lambda), IC50(nM) = 236.8 ± 10.6 against B.1.1.529 (Omicron) | |||
| 35455421 | 2022 | FLT | 163 | FN3 domain | Free | Linear | L | None | FN3 ,T1144 fusion protein | Antiviral (HIV fusion inhibitor) | Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested | 5.94 mg/kg | 27.09 ± 6.9 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | None | None | IC50(nM)= 65.3 ± 2.6 against HIV-1 96USSN20 (X4/R5, A), IC50(nM) = 9.8 ± 0.9 against HIV-1 96USNG17 (X4, A), IC50(nM) = 6.5 ± 0.2 against HIV-1 90US_873 (R5, B), IC50(nM) = 8.8 ± 0.3 against HIV-1 BZ167 (X4, B), IC50(nM) = 12.5 ± 0.5 against HIV-1 SE364 (R5, C), IC50(nM) = 9.3 ± 0.5 against HIV-1 PBL288 (R5, C), IC50(nM) = 11.7 ± 0.8 against HIV-1 92UG001 (X4/R5, D), IC50(nM) = 6.4 ± 0.3 against HIV-1 J32228M4 (R5, D), IC50(nM) = 7.5 ± 0.3 against HIV-1 DJ263 (R5, CRF02_AG), IC50(nM) = 10.2 ± 0.6 against HIV-1 CAM1475MV (R5, CRF02_AG) (Infection on MT-4 cells) | |||
| 35455421 | 2022 | T1144 | 37 | Free | Free | Linear | L | None | Fully or partially derived from the HIV-1 gp41 CHR domain | Antiviral (HIV fusion inhibitor) | Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested | 1.28 mg/kg | 7.48 ± 0.4 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | None | None | IC50(nM) = 3.9 against infection of HIV-1 IIIB (X4 tropic) strain | |||
| 35455421 | 2022 | T20 (enfuvirtide) | 36 | Free | Free | Linear | L | None | Derived from the natural sequence (aa 643–678) of the HIV-1 gp41 C-terminal heptad repeat (CHR) domain | Antiviral (HIV fusion inhibitor) | Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested | 1.26 mg/kg | 1.22 ± 0.2 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | None | None | IC50(nM)= 55.3 ± 2.4 against HIV-1 96USSN20 (X4/R5, A),IC50(nM) = 49.3 ± 4.9 against HIV-1 96USNG17 (X4, A), IC50(nM) = 50.1 ± 2.0 against HIV-1 90US_873 (R5, B), IC50(nM) =53.9 ± 4.3 against HIV-1 BZ167 (X4, B), IC50(nM) = 45.2 ± 3.2 against HIV-1 SE364 (R5, C), IC50(nM) = 46.9 ± 2.1 against HIV-1 PBL288 (R5, C), IC50(nM) = 77.1 ± 6.8 against HIV-1 92UG001 (X4/R5, D), IC50(nM) = 21.1 ± 1.1 against HIV-1 J32228M4 (R5, D), IC50(nM) = 55.6 ± 1.2 against HIV-1 DJ263 (R5, CRF02_AG), IC50(nM) = 61.2 ± 1.3 against HIV-1 CAM1475MV (R5, CRF02_AG) (infection on MT-4 cell) | |||
| 35438695 | 2022 | SFQSeM | 3 | Free | Selenium methylated conjugation at C terminal | Linear | L | None | From soybeans | Effective Se nutritional supplement | N.A. | N.A. | 81.60 ± 11.88 | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35430336 | 2022 | A6 peptide | 8 | Acetylation | Amidation | Linear | L | None | Synthetic | Antitumor | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35414877 | 2022 | B_3.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 347 | |||
| 35414877 | 2022 | B_3.2 | 25 | Acetylation | Amidation, FLAG tag | Linear | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | ~2 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 7890 | |||
| 35414877 | 2022 | B_1275 | 25 | Acetylation | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | ~3.5 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 2076 | |||
| 35414877 | 2022 | B_1275.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 1209 | |||
| 35414877 | 2022 | B_1275.2 | 25 | Acetylation | Amidation, FLAG tag | Linear | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | ~2 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 8336 | |||
| 35414877 | 2022 | B_1275.3 | 14 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 159 | |||
| 35414877 | 2022 | B_1275.4 | 25 | Acetylation | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 826 | |||
| 35414877 | 2022 | B_1275.5 | 14 | Acetylation | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 2300 | |||
| 35414877 | 2022 | B_1275.6 | 14 | C18 diacid-gGlu-2xOEG | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 860 | |||
| 35414877 | 2022 | Native GIP | 153 | Free | Free | Linear | L | None | Glucagon | Glucose dependent insulinotropic | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | 45 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | N.A. | |||
| 35414877 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | 35 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | PDB id: 5VAI | None | N.A. | |||
| 35414877 | 2022 | B_3.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 585 (Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 347 | |||
| 35414877 | 2022 | B_1275.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 643(Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 1209 | |||
| 35414877 | 2022 | B_1275.4 | 25 | Acetylation | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 3.767 (Elimination half life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 826 | |||
| 35414877 | 2022 | B_1275.5 | 14 | Acetylation | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 2.367 (Elimination half life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 2300 | |||
| 35414877 | 2022 | B_1275.6 | 14 | C18 diacid-gGlu-2xOEG | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 250 (Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 860 | |||
| 35359494 | 2022 | CSP1 | 17 | Free | Free | Linear | L | None | Competence stimulating peptide | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 30 | Trypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 10 for CSP1 against ComD1 receptor, EC50(nM) = 530 for CSP1 against ComD2 receptor | |||
| 35359494 | 2022 | CSP1 | 17 | Free | Free | Linear | L | None | Competence stimulating peptide | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 1 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 10 for CSP1 against ComD1 receptor, EC50(nM) = 530 for CSP1 against ComD2 receptor | |||
| 35359494 | 2022 | CSP1-E1A/F7Cha | 17 | Free | Free | Linear | L | introduction of Cha = cyclohexylalanine residues at position 7,E1A substituitions | CSP1 analog | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 4 | Trypsin | RP-HPLC | PBS solution | In Vitro | None | None | IC50(nM) = 36 for CSP1-E1A/F7Cha against ComD1 receptor | |||
| 35359494 | 2022 | CSP1-E1A/F7Cha | 17 | Free | Free | Linear | L | introduction of Cha = cyclohexylalanine residues at position 7 | CSP1 analog | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 4 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | IC50(nM) = 36 for CSP1-E1A/F7Cha against ComD1 receptor | |||
| 35359494 | 2022 | CSP1-F7Cha/I12Cha | 17 | Free | Free | Linear | L | introduction of Cha residues at positions 7 and 12 | CSP1 analog | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 3 | Trypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 0.97 for CSP1-F7Cha/I12Cha against ComD1 receptor, EC50(nM) = 70 for CSP1-F7Cha/I12Cha against ComD2 receptor | |||
| 35359494 | 2022 | CSP1-F7Cha/I12Cha | 17 | Free | Free | Linear | L | introduction of Cha residues at positions 7 and 12 | CSP1 analog | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 6 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 0.97 for CSP1-F7Cha/I12Cha against ComD1 receptor, EC50(nM) = 70 for CSP1-F7Cha/I12Cha against ComD2 receptor | |||
| 35180646 | 2022 | NPY1–36 | 36 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 4.66 ± 0.70 | Human plasma protease | LC-MS/MS | Human plasma after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY1–36 | 36 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 4.78 ± 1.07 | Human plasma protease | LC-MS/MS | Human plasma with 5 mg saxagliptin after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY3–36 | 34 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 26.9 ± 6.2 | Human plasma protease | LC-MS/MS | Human plasma after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY3–36 | 34 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 25.5 ± 6.2 | Human plasma protease | LC-MS/MS | Human plasma with 5 mg saxagliptin after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35174698 | 2022 | eGFP | 239 | Free | Free | Linear | L | None | Enhanced GFP | Tagging | N.A. | N.A. | 565 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Ec | 250 | GFP | Ec (E.coli) SsrA tag sequences conjugation | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 6 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Mf | 266 | GFP | Mf (M.fluorum) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 56 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | eGFP | 239 | Free | Free | Linear | L | None | Enhanced GFP | Tagging | N.A. | N.A. | No Degradation | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Ec | 250 | GFP | Ec (E.coli) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 14 | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Mf | 266 | GFP | Mf (M.fluorum) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 424 | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35150805 | 2022 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 1200 nmol/kg | 0.137 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.42nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-4aa-ABNF | 43 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 4 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 19.6 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 1.387 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-7aa'-ABNF | 46 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 7 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 20.8 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.5785 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-7aa-ABNF | 46 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 7 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 19.3 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.7459 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-12aa-ABNF | 51 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 12 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 21.9 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.8065 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-25aa-ABNF | 64 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 25 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 370 nmol/kg | 18.7 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.4903 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-Exenatide-4aa-ABNF | 82 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 4 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 300 nmol/kg | 20.5 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.3708 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35113575 | 2022 | TT1-IP peptide | 27 | Free | Amidation | Cyclic (C-C Disulfide Bond) | L | Conjugation of TT1 and IP proteins which is linked by Ahx | TT1 and IP fusion protein | Antitumor (Effect on TPP-IPs on Cll xenograft models) | periods of time (0, 1, 6, and 24 h) | 5 mg/kg | 40% of the peptide was recovered after 6 hours incubation | Human serum protease | MS using MALDI-TOF | Human serum | In Vitro | None | None | The average survival for TT1-IP and LinTT1-IP treated groups was 19 days (the survival range for TT1-IP group was 17-23 days and for LinTT1-IP group was 13-25 days) and for the control group 16 days (range of 14-20 days) | |||
| 35113575 | 2022 | TT1-IP peptide | 27 | Free | Amidation | Cyclic (C-C Disulfide Bond) | L | Conjugation of TT1 and IP proteins which is linked by Ahx | TT1 and IP fusion protein | Antitumor (Effect on TPP-IPs on Cll xenograft models) | plasma collected at 10, 20, 30, 45, 60, 120 and 360 min | 5 mg/kg | 28 (Terminal Half Life) | BALB/c mice plasma protease | HPLC-MS | Balb/c mice plasma | In Vivo | None | None | The average survival for TT1-IP and LinTT1-IP treated groups was 19 days (the survival range for TT1-IP group was 17-23 days and for LinTT1-IP group was 13-25 days) and for the control group 16 days (range of 14-20 days) | |||
| 35053417 | 2022 | (WR)8WK(Glutaryl-Dox)βA] | 19 | Free | βAlanine at C terminal conjugation | Cyclic | L | An ester bond is utilized to attach Dox with a glutaryl linker | Synthetic | Treat Breast, Leukemia, and Lymphoma Malignancies | 4 h at 37 °C | 5 µM | ∼6 | Human Serum Protease | HPLC | 25% Human serum | In Vitro | None | None | At 10 μM: 65% reduction in cell viability after 72 hours for SK-OV-3 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 19% cell viability after 72 hours for MDA-MB-231 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 77% reduction in cell viability after 72 hours for MCF-7 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 64% reduction in cell viability after 24 hours for MES-SA/MX2 Cells (DOX-resistant) Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ) | |||
| 35046019 | 2022 | ELP(0FA)GFP | 400 | Free | GFP | Linear | L | None | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 1.6 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA - Mouse serum albumin (μM) = n.d. (Binding affinity of ELP-GFP constructs for serum albumin), KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(1FA)GFP | 400 | Free | GFP | Linear | L | 1 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 1.9 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) = 126 ± 32.2, KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(5FA)GFP | 400 | Free | GFP | Linear | L | 5 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 19.6 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) = 10.3 ± 4.0, KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(10FA)GFP | 400 | Free | GFP | Linear | L | 10 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 33.3 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) =2.76 ± 0.19, KD HSA - Human serum albumin (μM) = n.d | |||
| 35046019 | 2022 | ELP(1FA)GFP | 400 | Free | GFP | Linear | L | 1 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 18.5 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) =25.9 ± 7.1, KD HSA - Human serum albumin (μM) = 19.3 ± 3.9 | |||
| 35046019 | 2022 | ELP(5FA)GFP | 400 | Free | GFP | Linear | L | 5 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 31.7 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) =4.0 ± 1.6, KD HSA - Human serum albumin (μM) = 3.16 ± 0.60 | |||
| 35046019 | 2022 | ELP(10FA)GFP | 400 | Free | GFP | Linear | L | 10 Fatty acid conjugation through pAzF (para-azidophenylalanine) | ELP-GFP conjugate | Increases Half Life | 1 week | 10 μM | 27.9 | C57Bl/6J mice blood plasma protease | GFP-specific ELISA | C57BL/6J mice blood plasma | In Vivo | None | None | KD MSA (μM) = 2.22 ± 0.03, KD HSA - Human serum albumin (μM) = 1.64 ± 0.17 | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 1 mg | 0.25 ± 0.02 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 4 mg | 0.36 ± 0.04 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 10 mg | 0.45 ± 0.05 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 20 mg | 0.55 ± 0.07 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 30 mg | 0.70 ± 0.08 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 45 mg | 0.73 ± 0.05 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 60 mg | 0.78 ± 0.06 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34910492 | 2022 | 68Ga-DOTA-SETSKSF | 7 | 68Ga labelled | Free | Cyclic | L | None | Synthetic | Used For Positron Emission Tomography imaging of PD-L1 expression in tumors | N.A. | N.A. | 14.48 ± 3.26 | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 34910492 | 2022 | 68Ga-DOTA-SETSKSF | 7 | 68Ga labelled | Free | Cyclic | L | None | Synthetic | Used For Positron Emission Tomography imaging of PD-L1 expression in tumors | N.A. | 5.29 ± 0.21 (%ID/g) | N.A. | N.A. | N.A. | H1975 tumor model | In Vitro | None | None | N.A. | |||
| 34910492 | 2022 | 68Ga-DOTA-SETSKSF | 7 | 68Ga labelled | Free | Cyclic | L | None | Synthetic | Used For Positron Emission Tomography imaging of PD-L1 expression in tumors | N.A. | 0.89 ± 0.10 (%ID/g) | N.A. | N.A. | N.A. | A549 tumor model | In Vitro | None | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.05 mg/kg | 7.37 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.125 mg/kg | 10.5 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.25 mg/kg | 19.94 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.25 mg/kg | 13.16 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.5 mg/kg | 16.2 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 1 mg/kg | 19.97 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 2.5 µg/kg | N.A. | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 7.5 µg/kg | N.A. | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 15 µg/kg | 24.4 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 30 µg/kg | 27 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at day 1 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 21 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at week 26 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 26.6 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at week 52, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 27.9 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34217775 | 2022 | FE 992326 | 30 | Free | Amidation | Linear | L | None | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min | 0.3 mg/kg | 6.5 ± 1.8 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992325 | 10 | D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Agp | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min | 0.3 mg/kg | 21 ± 2 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min | 0.2 mg/kg | 25 ± 8 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992326 | 30 | Free | Amidation | Linear | L | None | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min | 1 mg/kg | 11 ± 8.4 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992325 | 10 | D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Agp | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min | 1 mg/kg | 48 ± 11 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 40, 60, 90, 120, 180, 240, 300 min | 0.6 mg/kg | 23 ± 2 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min | 0.1 mg/kg | 82 ± 9 | Male göttingen minipigs plasma protease | LC-MS/MS | Male göttingen minipigs plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 40, 60, 90, 120, 180, 240, 300 min | 0.25 mg/kg | 264 ± 80 | Male göttingen minipigs plasma protease | LC-MS/MS | Male göttingen minipigs plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992325 | 10 | D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Agp | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min | 0.2 mg/kg | 69 ± 7 | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min | 0.1 mg/kg | 65 ± 5 | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 18.5 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 20 μg/kg | 7.87 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 17.1 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 500 μg/kg | 29.7 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 6 μg/kg | 5.27 ± 2.25 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 30 μg/kg | 19.6 ± 3.72 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 6 μg/kg | 20.0 ± 5.53 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 30 μg/kg | 25.5 ± 7.08 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 150 μg/kg | 29.3 ± 5.06 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| N.A. | 2022 | 12kD-PEG-e9-XPLGLAG-r9-k(cy5) | 25 | 12 KDa PEG | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 6 nmol | 20 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Alb-e9-XPLGLAG-r9-k(cy5) | 25 | Alb=albumin | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Alb=albumin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 4.8 nmol | 3 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Dex-e9-XPLGLAG-r9-k(cy5) | 25 | Dextran | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Dex=Dextran, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 5 nmol | 6 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Streptavidin-[e9-XPLGLAG-r9-k(cy5)]4 | 100 | Streptavidin | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Strep=Streptavidin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 4 nmol | 4 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | G5-PAMAM4-[e9-XPLGLAX-r9-k(cy5)]2[PEG]126 | 48 | G5-PAMAM4 | Cy5 linked with Lys side chain at C terminus, PEGylation | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Strep=Streptavidin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 3 nmol | 20 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Chem.37 (reference compound) | 33 | k=D-Lysine,Sar=N-terminal glycine, N£-octadecanoyl | Free | Linear | Mix | Aib substituitions at position 2 of semaglutide | Semaglutide Derivative | Antidiabetes | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 78 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | Test 1 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | GLP-1 analogs | Antidiabetes | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 100 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | Test 2 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | GLP-1 analogs | Antidiabetes | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 101 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | Test 3 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | GLP-1 analogs | Antidiabetes | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 105 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | Test 4 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | GLP-1 analogs | Antidiabetes | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 109 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 69 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | TROP2 TCE (PC1) | 692 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 3 ug/kg | 1.02 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | EC50(nM) = 0.1477 (TROP binding) | |||
| N.A. | 2022 | TROP2 TRACTr PC complex (PC5) | 911 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 ug/kg | 90.16 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | EC50(nM) = 60.25 (TROP binding) | |||
| N.A. | 2022 | TROP2 TRACTr PC complex (PC18) | 916 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 μg/kg | 97.31 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | IC50(pM) = 3,253 | |||
| N.A. | 2022 | TROP2 TRACTr PC complex (PC21) | 1177 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 μg/kg | 100.73 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | N.A. | |||
| N.A. | 2022 | PC-22 complex | 911 | Free | Fab heavy chain linked to C terminus of ScFv light chain | Linear | L | None | Synthetic | Mediates tumor cytotoxicity and T cell activation | N.A. | 100 μg/kg | 68.97 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | US 2021/0062261 W | N.A. | |||
| N.A. | 2022 | hIL-18BP | 194 | Free | Free | Linear | L | None | Synthetic | Antagonist of IL-18 | Single subcutaneous administration: 0, 0.33, 1, 1.5, 3, 5, 7, 12, 24, 48, 72, 120, And 168 Hours (13 Points In Total), Single Intravenous Administration: 0, 0.083, 0.25, 0.5, 1.25, 3, 5, 10, 24, 48, And 72 Hours (11 Points In Total) | 3 mg/kg + 1 mg/kg | 6.51 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | IB 2021058964 W | IC50 of IL-18BP-His was 0.0240 nM | |||
| N.A. | 2022 | hIL-18BP | 194 | Free | Free | Linear | L | None | Synthetic | Antagonist of IL-18 | Single intravenous administration: 0, 0.083, 0.25, 0.5, 1.25, 3, 5, 10, 24, 48, And 72 Hours (11 Points In Total) | 1 mg/kg | 6.51 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | IB 2021058964 W | IC50 of IL-18BP-His was 0.0240 nM | |||
| N.A. | 2022 | Example 12 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modification, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 46 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13 | |||
| N.A. | 2022 | Example 1 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG), B3E, B27E, B28E modifications, , A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 103 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 66.3 | |||
| N.A. | 2022 | Example 7 | 51 | Free | B29R, desB30 modificaiton | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 86 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 124.4 | |||
| N.A. | 2022 | Example 10 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 97 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3 | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 987 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 713 pmol/kg | 182 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1714 pmol/kg | 148 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 720 pmol/kg | 153 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 706 pmol/kg | 158 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1735 pmol/kg | 219 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 4 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A14E, A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B27E, B28E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 24 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 28.6 | |||
| N.A. | 2022 | Example 10 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modification, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 28 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3 | |||
| N.A. | 2022 | Example 11 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E, B28E modificatino, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 28 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13.6 | |||
| N.A. | 2022 | Example 12 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 25 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13 | |||
| N.A. | 2022 | PA2 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG) modifications | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 24 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | PA3 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B28D modifications | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 26 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 33 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 58 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 85.1 | |||
| N.A. | 2022 | Example 31 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B27E, B28E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 79 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 55 | |||
| N.A. | 2022 | Example 41 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 57 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 42 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 41 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | PA1 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG) modification | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 41 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| 35910276 | 2022 | KB-SP | 806 | Free | Free | Linear | L | None | Derived from Bacillus sp. KB111 strain | Haloprotease | 50°C | N.A. | 90 (Enzyme Activity) | N.A. | Zymography | EDTA + Tris-HCl + 0.5 M NaCl+ azocasein | In Vitro | GenBank id: KUL11341.1 | None | KB-SP exhibited more than 50% of the highest activity at pH=6.5–10 | |||
| 35910276 | 2022 | KB-SP | 806 | Free | Free | Linear | L | None | Derived from Bacillus sp. KB111 strain | Haloprotease | 60 °C | N.A. | 10 (Enzyme Activity) | N.A. | Zymography | EDTA + Tris-HCl + 0.5 M NaCl+ azocasein | In Vitro | GenBank id: KUL11341.1 | None | KB-SP exhibited more than 50% of the highest activity at pH=6.5–10 | |||
| 35910276 | 2022 | KB-SP | 806 | Free | Free | Linear | L | None | Derived from Bacillus sp. KB111 strain | Haloprotease | 50°C | N.A. | 5 (Enzyme Activity) | N.A. | Zymography | EDTA + Tris-HCl + 0.5 M NaCl+ azocasein | In Vitro | GenBank id: KUL11341.1 | None | KB-SP exhibited more than 50% of the highest activity at pH=6.5–10 | |||
| 35910276 | 2022 | BA17 | N.A. | Free | Free | Linear | L | None | Isolated from B. licheniformis | Serine protease | 50°C | N.A. | 90 (Enzyme Activity) | N.A. | Zymography | N.A. | In Vitro | None | None | N.A. | |||
| 35910276 | 2022 | BA17 | N.A. | Free | Free | Linear | L | None | Isolated from B. licheniformis | Serine protease | 60 °C | N.A. | 12 (Enzyme Activity) | N.A. | Zymography | N.A. | In Vitro | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38 (4A) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2CHSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 9.4, 37 °C | N.A. | 6 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38(4B) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2NSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 9.4, 37 °C | N.A. | 15.8 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38 (4A) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2CHSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 7.4, 37 °C, | N.A. | 600 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38(4B) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2NSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 7.4, 37 °C, | N.A. | 1580 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35711755 | 2022 | R13 Fae | 393 | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Xylanase | pH 6.0 25 Celsius | N.A. | 23 (Half Life Activty) | N.A. | N.A. | Phosphate buffer | In Vitro | None | None | N.A. | |||
| 35711755 | 2022 | R13 Fae | 393 | N.A. | N.A. | N.A. | N.A. | N.A. | Synthetic | Xylanase | pH 6.0 ,35°C | N.A. | 16 (Half Life Activity) | N.A. | N.A. | Phosphate buffer | In Vitro | None | None | N.A. | |||
| 35488338 | 2022 | FRAP-smTG | N.A. | Frap (A Fusion Tag) | Free | Linear | L | None | TGm1 variant | Used to generate protein crosslinking or attachment of small molecules | 60 ℃ | 0.4 mg/mL | < 2 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35488338 | 2022 | FRAP-TGm1 | N.A. | Frap (A Fusion Tag) | Free | Linear | L | None | TGm1 variant | Used to generate protein crosslinking or attachment of small molecules | 60 ℃ | 0.4 mg/mL | 11.31 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35488338 | 2022 | FRAPD-TGm1 | N.A. | Frap (A Fusion Tag) | Free | Linear | L | additional modification (Asp residue) | TGm1 variant | Used to generate protein crosslinking or attachment of small molecules | 60 ℃ | 0.4 mg/mL | 21.97 (Activity Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | 75°C | N.A. | 1.5 (Activity Half Life) | N.A. | N.A. | 10 mM CaCl2 at pH 9.0 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | 60°C | N.A. | 2 (Activity Half Life) | N.A. | N.A. | 10 mM CaCl2 at pH 11.0 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | N.A. | N.A. | >12 (Activity Half Life) | N.A. | N.A. | 10 mM CaCl2 at pH 7.5 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | mTSS | 436 | Free | Free | Linear | L | None | Derived from preTSS | Collagenolytic protease | 70°C | N.A. | 6 (Activity Half Life) | N.A. | N.A. | pH 9 | In Viro Study | None | None | In the presence of 10 mM CaCl2 at pH 9.0, mTSS retained more than 80% or 70% of the original activity after 8 h of incubation at 60°C or 70°C | |||
| 35133860 | 2022 | E187A | N.A. | Free | Free | Linear | L | Residue Glu187 of the Ca1 site in the catalytic domain was replaced by Ala | Derived from preTSS | Collagenolytic protease | 70°C | N.A. | N.A. | N.A. | N.A. | N.A. | In Viro Study | None | None | When the residue Glu187 of the Ca1 site in the catalytic domain was replaced by Ala, the resulting variant E187A was completely inactivated after incubation at 70°C for 3 h | |||
| 35177945 | 2022 | pE13F | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 7.2 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.56 ± 0.07 | |||
| 35177945 | 2022 | P26 | 12 | N-Acetylated Arg2 | Free | Linear | Mix | D-Leu, D-ala = l and a, Proline side chain linked with (4Br-Phe) at C terminus | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 86 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 2.11 ± 0.40 | |||
| 35177945 | 2022 | K17F | 17 | Free | Free | Linear | L | None | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 4.6 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.06 ± 0.01 | |||
| 35177945 | 2022 | P92 | 16 | Lys1 acetylation | Free | Linear | Mix | D-Arg = r, D-Gln = q, D-Leu = l, D-ala = a, Proline side chain linked with (4Br-Phe) at C terminus | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 24 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.09 ± 0.02 | |||
| 35177945 | 2022 | LIT01-196 | 17 | FC [CF3(CF2)7(CH2)2C(O)] conjugation at N terminal | Free | Linear | L | None | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 1440 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.08 ± 0.01 | |||
| 35177945 | 2022 | Apelin-13 | 13 | Free | Free | Linear | L | None | Secreted by White Adipose Tissue (Wat) in both humans and animals | Antidiabetes, Anorexic Effects | N.A. | N.A. | 2.1 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 7.4 x 10⁻⁹ M | |||
| 35177945 | 2022 | (Lys8GluPAL)apelin-13-amide | 13 | Free | Amidation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 1.2 x 10⁻¹⁰ M | |||
| 35177945 | 2022 | Lys8GluPAL(Tyr13)apelin-13 | 13 | Free | Tyr13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 1.1 x 10⁻⁹ M | |||
| 35177945 | 2022 | Lys8GluPAL(Val13)apelin-13 | 13 | Free | Val13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 2.2 x 10⁻¹⁰M | |||
| 35177945 | 2022 | pGlu(Lys8GluPAL)apelin-13-amide | 13 | pGlu = Pyroglutamate | Amidation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 3.1 x 10⁻¹⁰M | |||
| 35177945 | 2022 | Lys8GluPAL(Tyr13)apelin-13 | 13 | Free | Tyr13 modifcation, carboxylation | Linear | L | I125 radioactive labeled | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | Blood (20 microliter) collected at 0, 15, 30, 45, 60, 90, 120, 240, 480, 960 and 1440 min after injection | 4.1 nmol/kg | 2.5 - 3 | NIH swiss mice plasma protease | RP-HPLC | NIH swiss mice plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 1.1 x 10⁻⁹ M | |||
| 35177945 | 2022 | (Ala13)apelin-13 | 13 | Free | Ala13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 10.3 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.74e-009 (In vitro insulin secretion) | |||
| 35177945 | 2022 | (pGlu)apelin-13 | 13 | pGlu = Pyroglutamate | Amidation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 3.8 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.10e-008 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Ala13)apelin-13 | 13 | pGlu = Pyroglutamate | Ala13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 11.1 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 7.68e-009 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Val13)apelin-13 | 13 | pGlu = Pyroglutamate | Val13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic Activity | 0, 2, 4, 8, 24 h | 20 microgram | 9.8 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.59e-008 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Tyr13)apelin-13 | 13 | pGlu = Pyroglutamate | Tyr13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic Activity | 0, 2, 4, 8, 24 h | 20 microgram | 12.2 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.48e-008 (In vitro insulin secretion) | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 3.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 2.48 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 2.48 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 7.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.32 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 7.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.32 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 9.76 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 6.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 9.76 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 2.2 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.52 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 2.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.52 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 9.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 32.87 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 11.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 32.87 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 11.01 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 11.01 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.29 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.29 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 14 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 86.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 12.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 86.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 7.3 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 6.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 0.93 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 16.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 24.16 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) withheparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 8.68 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 6.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) withheparosan [HPN] | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 12.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 88.23 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.7 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 9.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 11.7 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35259149 | 2022 | Conjugate 2 | 31 | Free | Ethylene Diamine-modified chondroitin90 (CH) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | CH-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 25.3 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 9.9 nM | |||
| 35259149 | 2022 | Conjugate 2 | 31 | Free | Ethylene Diamine-modified chondroitin90 (CH) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | CH-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 100 nmol/kg | 30.3 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 9.9 nM | |||
| 35259149 | 2022 | Conjugate 3 | 31 | Free | Ethylene Diamine-modified heparosan (HPN) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | Hpn-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 33.6 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 7.0 nM | |||
| 35259149 | 2022 | Conjugate 3 | 31 | Free | Ethylene Diamine-modified heparosan (HPN) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | Hpn-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 100 nmol/kg | 25.8 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 7.0 nM | |||
| 35259149 | 2022 | TP5-MA | 5 | Free | Free | Linear | L | Conjugating a myristic acid-acylated lysine to a permissive site of TP5, Radiolabeling C14 at Lys2 | Myristic Acid-Modified Tp5 | Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids) | One hundred microliter plasma samples were collected at the following time intervals: 0.5, 5, 10, 20, 30, and 45 min and 1, 2, 3, 4, 6, 8,and 10 h after peptide administration. | 1 mg/kg | 1.75 ± 0.72 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5 | |||
| 35259149 | 2022 | TP5 | 5 | Free | Free | Linear | L | None | Synthetic | Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids) | One hundred microliter plasma samples were collected at the following time intervals: 0.5, 5, 10, 20, 30, and 45 min and 1, 2, 3, 4, 6, 8,and 10 h after peptide administration. | 1 mg/kg | 0.022 ± 0.004 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5 | |||
| 35259149 | 2022 | TP5-MA | 5 | Free | Free | Linear | L | Conjugating a myristic acid-acylated lysine to a permissive site of TP5, Radiolabeling C14 at Lys2 | Myristic Acid-Modified Tp5 | Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids) | 37 °C | N.A. | 4.42 | Human plasma protease | LC-MS/MS | 1 mg/mL human plasma | In Vitro | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 0.25 mg | 116 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 0.5 mg | 124 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 1 mg | 106 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 2.5 mg | 120 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 5 mg | 123 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 8 mg | 111 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35807558 | 2022 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety at Lys20 | Synthetic | Insulinotrophic | N.A. | 5 mg | 127 | Human plasma protease | N.A. | Human plasma With Multiple Dose (Participants Received 5‐Mg Tirzepatide Weeks 1‐8)(Japanese Participant With Type 2 Diabetes) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | N.A. | |||
| 35807558 | 2022 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety at Lys20 | Synthetic | Insulinotrophic | N.A. | 10 mg | 135 | Human plasma protease | N.A. | Human plasma With Multiple Dose (Participants Received 2.5‐Mg Tirzepatide, Weeks 1‐2; 5 Mg, Weeks 3‐4; 10 Mg, Weeks 5‐8) (Japanese Participant With Type 2 Diabetes) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | N.A. | |||
| 35807558 | 2022 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety at Lys20 | Synthetic | Insulinotrophic | N.A. | 15 mg | 121 | Human plasma protease | N.A. | Human plasma With Multiple Dose(Participants Received 5‐Mg Tirzepatide, Weeks 1‐2; 10 Mg, Weeks 3‐6; 15 Mg, Weeks 7‐8) (Japanese Participant With Type 2 Diabetes) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | N.A. | |||
| 35807558 | 2022 | PYY3-36 | 34 | Free | Free | Linear | L | None | Neuropeptide Y | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | PYY3−36 (methylamide) | 34 | Free | Methyl amide addition at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = >10,000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeTyr36]PYY3−36 | 34 | Free | Methylated Tyr36 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 370 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 4000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeArg35]PYY3−36 | 34 | Free | Methylated Arg35 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 620 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeGln34]PYY3−36 | 34 | Free | Methylated Gln34 at C terminus | Linear | L | Methylated Gln34 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 890 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 0.40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeArg33]PYY3−36 | 34 | Free | Methylated Arg33 at C terminus | Linear | L | Methylated Arg33 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 2500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoTyr36]PYY3−36 | 34 | Free | β-homoTyr36 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 430 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 4000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoArg35]PYY3−36 | 34 | Free | β-homoArg35 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 680 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 6300 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoGln34]PYY3−36 | 34 | Free | β-homoGln34 at C terminus | Linear | L | β-homoGln34 modification | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 1200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 160 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoArg33]PYY3−36 | 34 | Free | β-homoArg33 at C terminus | Linear | L | β-homoArg33 modification | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 230 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 200 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [Trp30, MeArg35]PYY3−36 | 34 | Free | MeArg35 at C terminus | Linear | L | Trp30 modification, Methylated Arg35 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 980 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 2500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [Trp30,β-homoArg35]PYY3−36 | 34 | Free | β-homoArg35 at C terminus | Linear | L | Trp30 modification | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 570 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 10,000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Treatment Of Type 2 Diabetes | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 46 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/, PDB id: 5VAI | None | N.A. | |||
| 35059568 | 2021 | JPE-1375 | 7 | Hoo = L-hydroorotic acid | Amidation | Linear | Mix | hle5 = D-homoleucine, Pff6 = Phe(4-F), Orn = Ornithine,Replaces the C-terminal Arg of PMX53 with a hydrophobic amino acid | Peptidomimetic C5a receptor antagonists | C5Ar1 Antagonists | Serial blood samples were collected at 10, 15, 30, 45, and 60 min, and at 2, 4, 6, and 24 h via a tail vein | 1 mg/kg | 0.13 (Elimination Half Life) | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | None | The inhibition of TNF levels also presented a similar median effective concentration (EC50) for PMX53 (5.9 μM) | |||
| 35059568 | 2021 | PMX53 | 6 | Acetylation | Free | Cyclic(Orn-Arg N-C bond) | Mix | cha4 = D-cyclohexylalanine, O2 = Ornithine | Peptidomimetic C5a receptor antagonists | C5Ar1 Antagonists | Serial blood samples were collected at 10, 15, 30, 45, and 60 min, and at 2, 4, 6, and 24 h via a tail vein | 1 mg/kg | 1.3 (Elimination Half Life) | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | None | The inhibition of TNF levels also presented a similar median effective concentration (EC50) for JPE-1375 (4.5 μM) | |||
| 35056979 | 2021 | Al-ProD | 4 | Maleimide | DOX | Linear | L | None | Albumin-binding maleimide and cathepsin B-cleavable peptide conjugate | Antitumor | blood samples were collected from mice at pre-determined times (0, 3 h, 6 h, 9 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h, and 144 h) | 3 mg/kg | 3.1 | BALB/C nude mice plasma protease | Fluorescence assay | BALB/c nude mice plasma | In Vivo | None | None | The IC50 value of HSA-bound Al-ProD in MDA-MB231 breast cancer cells is 7.33 µM, On day 20, the tumor volume in the Al-ProD-treated group was 347.42 ± 25.9 mm³, significantly smaller than the free DOX group (580.25 ± 139.92 mm³) and saline group (1810.98 ± 544.56 mm³) | |||
| 35036703 | 2021 | [64Cu]CM-1 | 13 | 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 1 hour | ∼100 μCi | 22.4 Of Intact [64Cu]Cm-1 Remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | CM1 shows high binding affinity for CD133 (KD = 7.37 nM), 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35036703 | 2021 | [64Cu]CM-1 | 13 | 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 2 hour | ∼100 μCi | 20.1% Of Intact [64Cu]Cm-1 Remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | CM1 shows high binding affinity for CD133 (KD = 7.37 nM), 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35036703 | 2021 | [64Cu]CM-2 | 14 | 6-aminohexanoic acid (Ahx) linker is anchored between the N terminus of the peptide and the (DOTA) 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid , 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 1 hour | ∼100 μCi | 94.9 of intact tracers remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35036703 | 2021 | [64Cu]CM-2 | 14 | 6-aminohexanoic acid (Ahx) linker is anchored between the N terminus of the peptide and the (DOTA) 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid , 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 2 hour | ∼100 μCi | 91.9% of intact tracers remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 2.35 mg/kg | 2.946 ± 2.048 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 4.7 mg/kg | 2.941 ± 1.399 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 9.4 mg/kg | 2.781 ± 1.021 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 4.7 mg/kg | 1.983 ± 0.583 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 34859381 | 2021 | M89b | 17 | pGlu = Pyroglutamate at position 1 | Free | Linear | L | None | galanin analog | Interacts With Different G Protein-Coupled Receptors | >23 hours | 10 µM | 40% Of M89B Had Been Degraded | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | EC50 ratios to Gal-(1-15)(n) = NA(3) (in GAL1R) (B-Arrestin), EC50 ratios to Gal-(1-15)(n) = NA(3) (in GAL1R) (Ca-efflux) | |||
| 34859381 | 2021 | GAL-(1–15) | 15 | Free | Free | Linear | L | None | isolated from the porcine intestine | Interacts With Different G Protein-Coupled Receptors | >30 minutes | 10 µM | 80% Of Gal-(1–15) Was Degraded | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | EC50 ratios to Gal-(1-15)(n) = 1.7(3) (in GAL2R) (B-Arrestin), EC50 ratios to Gal-(1-15)(n) = 1.4(3) (in GAL2R) (Ca-efflux) | |||
| 34707178 | 2021 | PYY3-36 analogues 1 | 34 | Free | Amidation | Linear | L | None | Derived from PYY | Antiobesity | Blood samples (0.8 ml) were taken either from the jugular vein using vacutainer or from the IV catheter not used for dosing according to one of the following schedules: Predose, and 5, 15, 30, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 192 h, 216 h, 240 h, 264 h and 288 h post dosing; or Predose, and 5, 30 min, 1 h, 2 h, 4 h, 7 h, 11 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 216 h, 264 h post dosing | 15 nmol/kg | 17 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.6 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 2 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 4 (C18 diacid-γGlu-2xAdo) | Derived from PYY | Antiobesity | Blood samples (0.8 ml) were taken either from the jugular vein using vacutainer or from the IV catheter not used for dosing according to one of the following schedules: Predose, and 5, 15, 30, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 192 h, 216 h, 240 h, 264 h and 288 h post dosing; or Predose, and 5, 30 min, 1 h, 2 h, 4 h, 7 h, 11 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 216 h, 264 h post dosing | 15 nmol/kg | 14 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 10 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 3 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 5 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 8.8 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 25 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 7 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 9 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 12 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 40 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 8 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 10 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 8.4 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 13 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 9 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 11 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 11 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 1.3 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 11 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 13 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 13 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 16 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 20 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 22 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 36 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 4 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 21 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 23 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 19 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 2 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 27 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 29 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 39 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 32 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 28 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 76 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 500 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 31 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 33 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 56 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 50 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 33 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 35 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 67 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 34 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 4 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 35 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 28 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 36 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 99 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 37 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 2 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 38 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 4 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 39 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 13 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 40 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 20 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 41 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 97 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 42 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 75 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 43 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 78 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 44 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 0.5 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 45 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 4, MeArg4 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 83 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 46 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 84 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 47 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 62 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 48 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 104 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 49 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 113 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 50 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 120 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 51 | 36 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 114 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 52 | 36 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 79 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 30 for Y2 receptor | |||
| 34661390 | 2021 | VVGS peptide | 15 | Free | Free | Linear | L | None | Synthetic | Targets tropoelastin | Aliquots (6 μL) taken after 0, 35, and 120 min | 0.6 mM which is diluted in water at a final concentration of 0.06 mM when aliquoting | 45 | Pooled serum protease from human male AB plasma | RP-HPLC | 50% pooled serum from human male AB plasma | In Vitro | None | None | KD (μM) = 41 ± 12 ( Interaction between Immobilized Human Recombinant Tropoelastin and Gd4TESMA) | |||
| 34661390 | 2021 | Gd4-TESMA | 19 | Gd4 | Free | Linear | L | Mal links KKK and other peptide | Synthetic | For imaging Atherosclerotic Plaque vulnerability | 2 hours | 0.6 mM which is diluted in water at a final concentration of 0.06 mM when aliquoting | No Degradation | Pooled serum protease from human male AB plasma | RP-HPLC | 50% pooled serum from human male AB plasma | In Vitro | None | None | KD (μM) = 41 ± 12 ( Interaction between Immobilized Human Recombinant Tropoelastin and Gd4TESMA) | |||
| 34630378 | 2021 | ABD-VP1 | 330 | ABD | Free | Linear | L | None | Synthetic | Treatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis | 1h at RT | 0.25 μg/μL | 280 | Murine serum protease | ELISA | Murine serum | In Vivo | None | None | ABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73% | |||
| 34630378 | 2021 | VP1 vaccine | 284 | Free | Free | Linear | L | None | Synthetic | Treatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis | 1h at RT | 0.25 μg/μL | <15 | Murine serum protease | ELISA | Murine serum | In Vivo | None | None | ABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73% | |||
| 34575581 | 2021 | C5a receptor 1 antagonist (PMX205) | 5 | HC = Hydrocinnamate, O1: ornithine | Free | Cyclic | Mix | D-Cha3: cyclohexylalanine | Lipophilic analogue of PMX53 | Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury | Blood samples were collected at 0.04, 0.25, 0.5, 0.75, 1, 1.5, 1, 4, 6, and 24 h for both groups and then 48, 72, 96, and 120 h | 1 mg/kg | 0.84 (Terminal Elmination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | IC50 = 31 nM for PMX205 | |||
| 34575581 | 2021 | C5a receptor 1 antagonist (PMX205) | 5 | HC = Hydrocinnamate, O1: ornithine | Free | Cyclic | Mix | D-Cha3: cyclohexylalanine | Lipophilic analogue of PMX53 | Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury | Samples (n = 4) were quenched at regular intervals of 5 min, 10 min, 15 min, 30 min and 60 min | 1 µg/ml | 0.17 (Elimination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | IC50 = 31 nM for PMX205 | |||
| 34575581 | 2021 | C5a receptor 1 antagonist (PMX205) | 5 | HC = Hydrocinnamate, O1: ornithine | Free | Cyclic | Mix | D-Cha3: cyclohexylalanine | Lipophilic analogue of PMX53 | Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury | Blood sample was collected at 2.5, 5, 10, 15, 30, 45, 60, and 90 min | 1 μg/mL | 0.33 (Elimination Half Life) | Mice spinal cord homogenate protease | LC-MS/MS | Mice spinal cord homogenate | In Vivo | None | None | IC50 = 31 nM for PMX205 | |||
| 34506138 | 2021 | α/sulfono-γ-AApeptide hybrid analogue 15 | 35 | Free | Amidation | Linear | L | Substitution of L-serine at position 2 with α-aminoisobutyric acid (Aib), X1 = Structure given in paper | α/Sulfono-γ-AApeptide Hybrid Analogues of Glucagon | Regulating glucose homeostasis | blood samples were obtained at 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h after injection | 5 mg/kg | ~4 | C57Bl/6J female mice plasma protease | LC-MS/MS | C57BL/6J female mice plasma | In Vivo | None | None | EC50 (nM) = 0.86 (Bioactivity of α/Sulfono-γ-AApeptide Hybrid Analogues in Cre Luc Production Functional Assay) | |||
| 34459035 | 2021 | FLAGHIF1α | 34 | Free | Free | Linear | L | FLAG tag | Hypoxia-Inducible Factor 1-alpha | Role in survival, metabolism, and angiogenesis | N.A. | N.A. | ~50% Increase | Cells lysate protease | CHX assay, Western blotting | HEK293 Flp‐In T‐REx cell lysate after pevonedistat treatment | In Vitro | PDB id: 1LQB | None | N.A. | |||
| 34459035 | 2021 | CODD | 120 | Free | Free | Linear | L | FLAG tag | C-Terminal oxygen-dependent degradation domain | Regulates gene expression | N.A. | N.A. | 5.8‐Fold Increase | Cells lysate protease | CHX assay, Western blotting | HEK293 Flp‐In T‐REx cells lysate after neddylation inhibition | In Vitro | None | None | N.A. | |||
| 34455010 | 2021 | ELA-32 | 32 | pGlu = Pyroglutamate | Free | Cyclic (Cys-Cys Disulfide Bond) | L | None | Derived from Zebrafish | Anticancer, Treatment of Cardiovascular Disease | Blood sample were withdrawn at time points: 0, 2, 5, 10, 15, 30, 60, 120, 240 min | 5 μg/mL | 47.2 ± 5.7 | Human plasma protease | LC–MS/MS | Human plasma | In Vitro | None | None | N.A. | |||
| 34455010 | 2021 | ELA-32 | 32 | pGlu = Pyroglutamate | Free | Cyclic (Cys-Cys Disulfide Bond) | L | None | Derived from Zebrafish | Anticancer, Treatment of Cardiovascular Disease | Blood sample were withdrawn at time points: 0, 2, 5, 10, 15, 30, 60, 120 min | 5 μg/mL | 44.2 ± 3 | Human kidney homogenate protease | LC–MS/MS | Human kidney homogenate | In Vitro | None | None | N.A. | |||
| 34450223 | 2021 | GLP-2DARPin | 31 | Genetic fusion of modified GLP-1 to the N-terminal of DARPins through a flexible linke (GGGGS)3 further DARPin linked with another DARPin using PT-linker | Free | Linear | L | FITC labeled | GLP-1 analogs | Antidiabetes | At 0.5, 2, 4, 7, 10, 24, 36, 48 and 72 h after injection, 20 μL of blood was collected | 2 mg/mL | 52.3 ± 4.6 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Glucose-lowering effect of GLP-DARPin was more potent than that of GLP-2DARPin, EC50 of GLP-2DARPin was 0.51 ± 0.04 nM | |||
| 34450223 | 2021 | GLP-DARPin | 31 | Genetic fusion of modified GLP-1 to the N-terminal of DARPins through a flexible linke (GGGGS)3 | Free | Linear | L | FITC labeled | GLP-1 analogs | Antidiabetes | At 0.5, 2, 4, 7, 10, 24, 36, 48 and 72 h after injection, 20 μL of blood was collected | 2 mg/mL | 18.0 ± 2.8 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Glucose-lowering effect of GLP-DARPin was more potent than that of GLP-2DARPin, EC50 of GLP-2DARPin was 9.06 ± 0.15 nM | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1.1 | Human plasma protease | N.A. | Human adult plasma (in Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1.24 | Human plasma protease | N.A. | Human adult plasma (in Non-Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 0.89 | Human plasma protease | N.A. | Human pediatrics plasma (in Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1 | Human plasma protease | N.A. | Human pediatrics plasma (in non - Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34393794 | 2021 | LIT01-196 | 17 | Fluorocarbon chain (CF3(CF2)7(CH2)2C(O)) attached to the N-terminal part of K17F | Free | Linear | L | None | Apelin-17 Analog | Treatment of Hypertension | N.A. | 15 nmol/kg | 156 | Rats plasma protease | RIA | Rats plasma | In Vivo | Pubchem CID Apelin: 56841713 | None | IC50 = 0.56 ± 0.04 nmol/l for LIT01-196 | |||
| 34393794 | 2021 | K17F | 17 | Free | Free | Linear | L | None | Apelin-17 Analog | Treatment of Hypertension | N.A. | 250 nmol/kg | 50 | Rats plasma protease | RIA | Rats plasma | In Vivo | Pubchem CID Apelin: 56841713 | None | IC50: 0.11 ± 0.01 nmol/l for K17F | |||
| 34393794 | 2021 | LIT01-196 | 17 | Fluorocarbon chain (CF3(CF2)7(CH2)2C(O)) to the N-terminal part of K17F | Free | Linear | L | None | Apelin-17 Analog | Treatment of Hypertension | N.A. | 900 nmol/kg | 28 | Rats plasma protease | RIA | Rats plasma | In Vivo | Pubchem CID Apelin: 56841713 | None | IC50 = 0.56 ± 0.04 nmol/l for LIT01-196 | |||
| 34358122 | 2021 | AT1-HSA-MRN-NPs | 12 | Free | HSA linked through PEG4 | Linear | L | None | Synthetic | Treatment of Cardiovascular Disease | Blood was collected from the jugular vein at the following timepoints: 0, 5, 15, 30, 45, 60, 120, and 360 min | 50 μg/kg | 101.3 | Rats plasma protease | HPLC | Rats plasma | In Vivo | None | None | N.A. | |||
| 34254101 | 2021 | Glycylglycine model dipeptide | 2 | Free | Free | Linear | L | None | Synthetic | N.A. | 60 °C and pD 7.4 | Equimolar amounts of Hf-NU-1000 and GG | 231 | N.A. | 1H-NMR | Equimolar amounts of Hf-NU-1000 (Metal-organic Framework)(Hf6O8-based NU-1000) and GG | In Vitro | None | None | A glycylglycine model dipeptide was hydrolysed with a rate constant of kobs = 8.33 × 10−7 s−1 | |||
| 34206631 | 2021 | Leu-ENK | 5 | Free | Free | Linear | L | None | Opioid peptide | Analgesic | Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min | 315 µmol/L | 25 | Mice plasma protease | UPLC | Mice dipotassium ethylenediaminetetraacetic acid containing pooled plasma | In Vitro | None | None | N.A. | |||
| 34206631 | 2021 | KK 103 | 6 | N terminal of Tyr linked with NH bond with R1 = Structure given in paper | Free | Linear | L | None | Synthetic | Analgesic | Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min | 315 µmol/L | 37 | Mice plasma protease | UPLC | Mice dipotassium ethylenediaminetetraacetic acid containing pooled plasma | In Vitro | None | None | N.A. | |||
| 34206631 | 2021 | KK 103 | 6 | N terminal of Tyr linked with NH bond with R1 = Structure given in paper | Free | Linear | L | None | Synthetic | Analgesic | Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min | 315 µmol/L | >95% Remained | CSF Protease | UPLC | Pooled human cerebrospinal fluid | In Vitro | None | None | N.A. | |||
| 34206631 | 2021 | Leu-ENK | 5 | Free | Free | Linear | L | None | Opioid peptide | Analgesic | Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min | 315 µmol/L | >80% Remained | CSF Protease | UPLC | Pooled human cerebrospinal fluid | In Vitro | None | None | N.A. | |||
| 34201398 | 2021 | optP7 | 9 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | For 0, 0.5, 1, 3, 6, and 24 h at 37 °C | 100 μM | 13 | Human serum protease | UPLC-MS | Human serum | In Vitro | None | None | MIC(µM) = 3 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 0.8 for E.coli in growth media MH,MIC(µM) = 1.5 for K. pneumoniae in growth media MH,MIC(µM) = 1.5 for A. baumannii in growth media MH,MIC(µM) = 0.8 for VRE in growth media MH,MIC(µM) = 6 for MRSA in growth media MH | |||
| 34201398 | 2021 | c-optP7 | 15 | Free | Free | Cyclic(Cys1-Cys15) | L | All Alanine replaced by β-alanine | Synthetic | Antimicrobial | For 0, 0.5, 1, 3, 6, and 24 h at 37 °C | 100 μM | 9 | Human serum protease | UPLC-MS | Human serum | In Vitro | None | None | MIC(µM) = 142 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 71 for E.coli in growth media MH,MIC(µM) > 142 for K. pneumoniae in growth media MH,MIC(µM) = ND for A. baumannii in growth media MH,MIC(µM) > 142 for VRE in growth media MH,MIC(µM) = 142 for MRSA in growth media MH | |||
| 34201398 | 2021 | [L6-optP7]-Mco | 35 | Free | Free | Cyclic(Cys-Cys Multiple Disulfide Loops) | L | None | Synthetic | Antimicrobial | For 0, 0.5, 1, 3, 6, and 24 h at 37 °C | 100 μM | 435 | Human serum protease | UPLC-MS | Human serum | In Vitro | None | None | MIC(µM) = 62 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 62 for E.coli in growth media MH,MIC(µM) = 62 for K. pneumoniae in growth media MH,MIC(µM) = 62 for A. baumannii in growth media MH,MIC(µM) > 62 for VRE in growth media MH,MIC(µM) > 62 for MRSA in growth media MH | |||
| 34163352 | 2021 | OPT | 20 | Free | Free | Linear | L | None | Derived from the QKHPD-containing region of NCX1 | Binds To Pser68-Plm | Aliquots of 50 μl were collected at different time points (0–48 h) | 300 μM | 0.86 | Human serum protease | Mass spectrometry | Human serum | In Vitro | None | None | N.A. | |||
| 34163352 | 2021 | NOPT | 16 | OPT substituted with an N-methyl proline at position 1 | Free | Linear | L | None | Derived from OPT | Binds To Pser68-Plm | Aliquots of 50 μl were collected at different time points (0–48 h) | 300 μM | 14.9 | Human serum protease | Mass spectrometry | Human serum | In Vitro | None | None | N.A. | |||
| 34122400 | 2021 | CATH2 | 27 | Free | Free | Linear | L | None | Cationic chicken heterophil-derived peptide | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 302 ± 34.5 | Human serum protease | HPLC | Human serum | In Vitro | None | None | The cytotoxicity of CbTP was lower than that of parental peptide CATH2 | |||
| 34122400 | 2021 | TP5 | 5 | Free | Free | Linear | L | None | derived from thymopoietin | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 3.2 ± 0.5 | Human serum protease | HPLC | Human serum | In Vitro | None | None | The cytotoxicity of CbTP was lower than that of parental peptide CATH2 | |||
| 34122400 | 2021 | CbTP | 18 | Free | TP5 conjugation | Linear | L | None | A hybrid peptide combining TP5 and fragments of CATH2 | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 353 ± 41.3 | Human serum protease | HPLC | Human serum | In Vitro | None | None | CbTP induced cytotoxicity in a dose-dependent manner, while even a high dose (80 µg/mL) of CbTP was nontoxic to RAW264.7 cells | |||
| 34064291 | 2021 | 111In-DOTA-EB-cRGDfK | 5 | Radiolabelled with 111ln, DOTA, EvansBlue dye | Free | Cyclic | L | None | Synthetic | For Spect imaging and potential theranostic | Blood samples (10 μL) were collected by heart puncture under 2% isoflurane anesthesia at 0.083, 0.5, 2, 4, 24, 48, 72, 96, and 168 h | 1.85 MBq | 77.3 (Terminal Half Life) | U-87 mg tumor bearing mice plasma protease | Radioactivity assay | U-87 mg tumor-bearing mice plasma | In Vivo | None | None | IC50(nM) =71.7 | |||
| 34064291 | 2021 | 111In-DOTA-cRGDfK | 5 | Radiolabelled with 111ln, DOTA | Free | Cyclic | L | None | Synthetic | For Spect imaging and potential theranostic | Blood samples (10 μL) were collected by heart puncture under 2% isoflurane anesthesia at 0.083, 0.5, 2, 4, 24, 48, 72, 96, and 168 h | 1.85 MBq | 17.2 (Terminal Half Life) | U-87 mg tumor bearing mice plasma protease | Radioactivity assay | U-87 mg tumor-bearing mice plasma | In Vivo | None | None | IC50(nM) =35.2 | |||
| 36133017 | 2021 | Fab–CKP-NLP | 30 | Free | Free | Linear | L | Fab conjugation, Lys1 fatty acid conjugation (Palm) | Synthetic | Platform for potential delivery of peptide like drug candidates | 37 °C for 24 hour | N.A. | 75% Remained Intact | N.A. | SEC | N.A. | In Vitro | None | None | N.A. | |||
| 36133017 | 2021 | CKP-NLP | 30 | Free | Free | Linear | L | AF488 labeled , Lys1 fatty acid conjugation (Palm) | Synthetic | Platform for potential delivery of peptide like drug candidates | 37 °C | N.A. | 1 | N.A. | SEC | N.A. | In Vitro | None | None | N.A. | |||
| 34048741 | 2021 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Salivary gland of the lizard Heloderma suspectum | Antidiabetes | Blood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h | 0.07 mg/kg | 0.32 ± 0.04 | Male SD rats plasma protease | ELISA | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 34048741 | 2021 | M4 | 40 | Free | Cys addition at C terminal | Linear | L | M, R amino acid substitutions | Synthetic | Antidiabetes | Blood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h | 0.07 mg/kg | 1.80 ± 0.23 | Male SD rats plasma protease | ELISA | Male SD rats plasma | In Vivo | None | None | EC50(nM) = 38.49 ± 4.58 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 33969456 | 2021 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples for PK assessment were obtained during the first 9 days of dosing (7–45 samples per subject) and following the last dose on day 10 (16–38 samples per subject) | N.A. | 158 | Human plasma protease | LC-MS | Human plasma (Healthy subjects) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/ | None | N.A. | |||
| 33969456 | 2021 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples for PK assessment were obtained during the first 9 days of dosing (7–45 samples per subject) and following the last dose on day 10 (16–38 samples per subject) | N.A. | 146 | Human plasma protease | LC-MS | Human plasma (Subjects with T2D) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/ | None | N.A. | |||
| 33940058 | 2021 | OPBP-1 | 12 | Free | Free | Linear | D | Substituition of A with Y at position 10 | Derived from H12 | Anticancer | Co-incubation of OPBP-1 with 10% human serum for 0 h, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, 32 h and 48 h. | 8 mg/kg | 0.33 ± 0.01 | Male SD rats plasma protease | RP-HPLC | Male SD rats plasma | In Vivo | None | None | After 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models. | |||
| 33940058 | 2021 | OPBP-1 | 12 | Free | Free | Linear | D | Substituition of A with Y at position 10 | Derived from H12 | Anticancer | Co-incubation of OPBP-1 with 10% human serum for 0 h, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, 32 h and 48 h. | 20 mg/kg | 8.69 ± 1.19 | Male SD rats plasma protease | RP-HPLC | Male SD rats plasma | In Vivo | None | None | After 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models. | |||
| 33940058 | 2021 | OPBP-1@TMC | 12 | Free | Free | Linear | D | Substituition of A with Y at position 10 | Derived from H12 | Anticancer | Co-incubation of OPBP-1 with 10% human serum for 0 h, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, 32 h and 48 h. | 20 mg/kg | 14.55 ± 1.43 | Male SD rats plasma protease | RP-HPLC | Male SD rats plasma | In Vivo | None | None | After 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models. | |||
| 33918853 | 2021 | HFn/DOX | 172 | Free | Free | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 3.07 ± 0.06 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.49 ± 0.11 | |||
| 33918853 | 2021 | HFn-PAS/DOX | 235 | Free | 15aa linker, enzyme cleavable site, PAS(40), 5 aa flexible linker conjugated at C terminus | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 14.96 ± 0.29 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.38 ± 0.09 | |||
| 33918853 | 2021 | HFn-GFLG-PAS-RGDK/DOX | 239 | Free | Add RGDK tretapeptide to HFn-PAS C-terminus | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 17.61 ± 0.39 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.17 ± 0.01 | |||
| 33918853 | 2021 | HFn-PLGLAG-PAS-RGDK/DOX | 241 | Free | Add RGDK tretapeptide to HFn-PAS C-terminus and substituite enzyme cleavable linker with PLGLAG | Linear | L | None | Synthetic | Antitumor | Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C | 3.0 mg/kg | 18.93 ± 0.61 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.18 ± 0.04 | |||
| 33894838 | 2021 | Cagrilintide | 37 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | Mix | LPPTNVGSNTP all D-amino acids, Lipidation on Lys1 | amylin analogue | Antiobesity | Blood samples for pharmacokinetic testing were collected before dosing at baseline (week 0) and at weekly visits, and after the last dose (week 19) at 4, 8, 12, 24, 48, 72, 96, 168, 336, 504, 672, 840, and 1008 h after dosing | 0·16 − 4·5 mg | 159 – 195 | Human plasma protease | N.A. | Human plasma | In Vivo | pubchem CID: 171397054 | None | N.A. | |||
| 33894838 | 2021 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples for pharmacokinetic testing were collected before dosing at baseline (week 0) and at weekly visits, and after the last dose (week 19) at 4, 8, 12, 24, 48, 72, 96, 168, 336, 504, 672, 840, and 1008 h after dosing | 2·4 mg | 145 – 165 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 33825469 | 2021 | Native Ex4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 0.72 ± 0.07 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33825469 | 2021 | FITC-labeled Ex4−DNP 9 | 44 | FITC-Ahx | Ex4 linked to DNP9 = Dinitro phenol by (PEG)n spacer | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 2.07 ± 0.05 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33825469 | 2021 | FITC-labeled Ex4−DNP 10 | 44 | FITC-Ahx | Ex4 linked to DNP10 = Dinitro phenol by (PEG)n spacer | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 3.55 ± 0.33 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33825469 | 2021 | FITC-labeled Ex4−DNP 11 | 44 | FITC-Ahx | Ex4 linked to DNP11 = Dinitro phenol by (PEG)n spacer | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 2.62 ± 0.17 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 6C | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 87 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 6C | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 87 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 6C | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 1030 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 7 | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 256 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 7 | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 724 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 7 | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 2490 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 8 | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a four-carbon spacer between the β-carbon and the triazole, Mod = MeSO2−, X = Structure given in paper (n=2) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 1570 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33822591 | 2021 | PEG−DNP-Lys conjugates 8 | 1 | DNP | PEG20 KDa, MeO | Linear | L | GDM linker with a four-carbon spacer between the β-carbon and the triazole, Mod = MeSO2−, X = Structure given in paper (n=2) | Synthetic | Increases Half Life | pH 7.4 | N.A. | 5310 (b-Elimination Half-Life) | N.A. | N.A. | N.A. | In Vitro | None | None | N.A. | |||
| 33813091 | 2021 | FITC-TPP1 | 21 | FITC labelled | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding | 4 mg/kg | <10 (Blood Clearance Half Life) | Mice blood plasma protease | Fluorescence spectrometry | Mice blood plasma | In Vivo | None | None | N.A. | |||
| 33813091 | 2021 | TPP1 (SPIO NP@M-P) | 21 | FITC labelled | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding | 4 mg/kg | 6 (Blood Clearance Half Life) | Mice blood plasma protease | Fluorescence spectrometry | Mice blood plasma | In Vivo | None | None | N.A. | |||
| 33791863 | 2021 | 125I-Ang1–7 | 7 | Free | Free | Linear | L | 125I labeled | Synthetic | Role in Renal and Cardiovascular Homeostasis | Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration | 4.5 mM | 0.6 | Rats plasma protease | Radioactivity assay | Rats plasma | In Vivo | None | None | Ang1–7 exhibited 4.2±0.1%, 3.7±0.6%, 4.4±0.2%, and 2.6±0.4% binding capacity in D.D. water, PBS 50 mM, PBS10mM, and acetate bufer, respectively | |||
| 33791863 | 2021 | 125I-Ang Conj. | 7 | Thiol bisphosphonate,Maleimidopropionyl,PEG conjugated at N terminus | Free | Linear | L | 125I labeled | Synthetic | Role in Renal and Cardiovascular Homeostasis | Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration | 4.5 mM | 3.4 | Rats plasma protease | Radioactivity assay | Rats plasma | In Vivo | None | None | Ang Conj. values were 20.4±0.5%,6.8±0.6%, 8.4±0.2%, and 11.6±0.2% | |||
| 33791863 | 2021 | 125I-Ang Conj | 7 | Thiol bisphosphonate,Maleimidopropionyl,PEG conjugated at N terminus | Free | Linear | L | 125I labeled | Synthetic | Role in Renal and Cardiovascular Homeostasis | Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration | 4.5 mM | 6.6 | Rats plasma protease | Radioactivity assay | Rats plasma | In Vivo | None | None | Ang Conj. values were 20.4±0.5%,6.8±0.6%, 8.4±0.2%, and 11.6±0.2% | |||
| 33706686 | 2021 | TB01-3 | 39 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | 250 ul blood samples were collected via jugular vein cannula at these time points: pre-dose, 0.0833, 0.25, 0.5, 1, 2, 4, 8, 24, 48, 72, 96, 168, 240 and 336 hours post dose. | 10 mg/kg | ~1 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | TB59-2 binds specifically to the GLP-1 R with an EC50 of 15.5 nM, TB-59-2 is a potent agonist in the cAMP assay with a similar EC50 as the GLP-1 7–36 peptide, TB59-2 can also induce the β-arrestin recruitment in GLP-1 R expression cells | |||
| 33706686 | 2021 | TB59-2 | 30 | GLP-1 7–36 peptide is linked to the light chain N-terminal of the TB01-2 antibody via a (G4S)x3 linker | Free | Linear | L | None | Synthetic | Antidiabetes | 250 ul blood samples were collected via jugular vein cannula at these time points: pre-dose, 0.0833, 0.25, 0.5, 1, 2, 4, 8, 24, 48, 72, 96, 168, 240 and 336 hours post dose. | 10 mg/kg | >2 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | TB59-2 binds specifically to the GLP-1 R with an EC50 of 15.5 nM, TB-59-2 is a potent agonist in the cAMP assay with a similar EC50 as the GLP-1 7–36 peptide, TB59-2 can also induce the β-arrestin recruitment in GLP-1 R expression cells | |||
| 33674401 | 2021 | 177Lu-DOTA-LM3 | 9 | DOTA | Amidation | Cyclic(C-C NC terminal bond) | Mix | DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine | SST analog | Treating Metastatic Neuroendocrine Neoplasms (Nens) | N.A. | 7 ± 1 GBq | 76 | Whole body | Dosimetry | whole body | In Vivo | None | None | Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms ) | |||
| 33674401 | 2021 | 177Lu-DOTA-LM3 | 9 | DOTA | Amidation | Cyclic | Mix | DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine | SST analog | Treating Metastatic Neuroendocrine Neoplasms (Nens) | N.A. | 7 ± 1 GBq | 92 | Human kidney homogenate protease | Dosimetry | Human kidney homogenate | In Vivo | None | None | Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms ) | |||
| 33674401 | 2021 | 177Lu-DOTA-LM3 | 9 | DOTA | Amidation | Cyclic | Mix | DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine | SST analog | Treating Metastatic Neuroendocrine Neoplasms (Nens) | N.A. | 7 ± 1 GBq | 97 | Human spleen | Dosimetry | Human spleen | In Vivo | None | None | Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms ) | |||
| 33674401 | 2021 | 177Lu-DOTA-LM3 | 9 | DOTA | Amidation | Cyclic | Mix | DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine | SST analog | Treating Metastatic Neuroendocrine Neoplasms (Nens) | N.A. | 7 ± 1 GBq | 111 | Human metastases | Dosimetry | Human metastases | In Vivo | None | None | Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms ) | |||
| 33672039 | 2021 | GLP1_8G37C-HSA | 31 | Free | HSA | Linear | L | Substituition of amino acid G at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 3.2 (T1/2a) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50= 1340 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33672039 | 2021 | GLP1_8A37C-HSA | 30 | Free | HSA | Linear | L | Substituition of amino acid A at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 3.3 (T1/2a) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50=185 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33672039 | 2021 | GLP1_8G37C-HSA | 31 | Free | HSA | Linear | L | Substituition of amino acid G at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 9 ( T1/2b) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50= 1340 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33672039 | 2021 | GLP1_8A37C-HSA | 30 | Free | HSA | Linear | L | Substituition of amino acid A at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 7.1 (T1/2b) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50=185 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33665501 | 2021 | PLG-Pt | n | Free | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | None | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 1.9 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 4.8 in SKOV3 cells | |||
| 33665501 | 2021 | PEG-PLG-Pt | n | PEGylation | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | PEGylation | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 8.8 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 11 in SKOV3 cells | |||
| 33665501 | 2021 | PEG-pHe-PLG-Pt (pH 7.4) | n | PEG-CDM | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | Poly(L-glutamic acid) is grafted with methoxy poly(ethylene glycol) (PEG) using a pH-sensitive linker, 2-propionic-3-methylmaleic anhydride = CDM | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 7.9 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 8.5 in SKOV3 cells | |||
| 33665501 | 2021 | PEG-pHe-PLG-Pt (pH 6.5) | n | PEG-CDM | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | Poly(L-glutamic acid) is grafted with methoxy poly(ethylene glycol) (PEG) using a pH-sensitive linker, CDM = 2-propionic-3-methylmaleic anhydride | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | N.A. | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 5.8 in SKOV3 cells | |||
| 33665501 | 2021 | PEG-MMP-PLG-Pt | n+6 | PEGylation | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | PEGylation through an MMP-sensitive peptide linker (PLGLAG), CDM = 2-propionic-3-methylmaleic anhydride | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 7.8 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 6.9 in SKOV3 cells | |||
| 33656323 | 2021 | IL-2 | 132 | Free | Free | Cyclic (C57-C104 Disulfide Bond) | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.041 ± 0.006 (T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.613 ± 0.063(T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 control | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.035 ± 0.014(T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | IL-2 | 132 | Free | Free | Cyclic (C57-C104 Disulfide Bond) | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.273 ± 0.040(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 3.595 ± 0.518(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 control | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.196 ± 0.114(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33650155 | 2021 | 3XFLAG-hDASPO_341 | 365 | 3XFLAG labelling | Free | Linear | L | None | Found in the hippocampus of female patients affected by Alzheimer's disease | Degradation Of D-Aspartate ( D-Asp) | 10 hours | 2 μg | ≈ 100 | U87 cells lysate protease | Western blotting | U87 cells lysate with cycloheximide (CHX) | In Vivo | None | None | N.A. | |||
| 33650155 | 2021 | 3XFLAG-hDASPO_369 | 393 | 3XFLAG labelling | Free | Linear | L | None | Found in the hippocampus of female patients affected by Alzheimer's disease | Degradation Of D-Aspartate ( D-Asp) | 10 hours | 2 μg | ≈ 100 | U87 cells lysate protease | Western blotting | U87 cells lysate with cycloheximide (CHX) | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 1 mg | 0.26 ± 0.02 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 4 mg | 0.36 ± 0.04 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 10 mg | 0.45 ± 0.05 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 20 mg | 0.55 ± 0.07 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 30 mg | 0.70 ± 0.08 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 45 mg | 0.73 ± 0.05 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 60 mg | 0.78 ± 0.06 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607165 | 2021 | NT(8:13) | 6 | Free | Free | Linear | L | None | Neuropeptide | Analgesic | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 0.98 ± 0.08 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 1.65 ± 0.06 for hNTS1 | |||
| 33607165 | 2021 | JMV438 | 6 | Both Arg residues in positions 1 and 2 were replaced by two Lys | Free | Linear | L | None | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 1.57 ± 0.27 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 4.00 ± 0.35 for hNTS1 | |||
| 33607165 | 2021 | JMV449 | 6 | Free | Free | Linear | L | Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9 | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 8.37 ± 2.02 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 2.02 ± 0.80 for hNTS1 | |||
| 33607165 | 2021 | JMV5170 | 6 | Free | Free | Linear | L | Pro10 was then substituted by the silylated proline analog silaproline(Sip) , Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9 | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 22.1 ± 1.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 296 ± 51 for hNTS1 | |||
| 33607165 | 2021 | JMV5206 | 6 | Free | substitution of Leu13 by the (L)-(Trimethylsilyl)-Alanine (TMSAla) | Linear | L | Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9 | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 2.13 ± 0.19 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 2.45 ± 0.17 for hNTS1 | |||
| 33607165 | 2021 | JMV5296 | 6 | Free | Free | Linear | L | Di-substitution with both Sip and TMSAla, Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9 | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 20.6 ± 4.15 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 610 ± 31 for hNTS1 | |||
| 33555858 | 2021 | B10-33 (Cpd 58) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with(-(γE)3-C16), Aib | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 4.3 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 17.6 ± 8.1(97%) in OVCAR5 cells | |||
| 33555858 | 2021 | B10-33 (Cpd 59) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C16), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 8.9 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 3.6 ± 2.0 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 60(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C16), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 6.4 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 3.2 ± 2.1 (74%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 61(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 4.8 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 1.0 ± 0.9 (79%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 62(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 4.3 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.6 ± 0.4 (95%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 63(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C16), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 5.7 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 1.0 ± 0.6 (80%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 64(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 3.9 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.2 ± 0.1 (89%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 65(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 3.4 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.1 ± 0.1 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 66(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 3.96 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.4 ± 0.2 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 67(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C16-OH), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | N.A. | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 809 ± 20 (70%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 68(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C18-OH), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | N.A. | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 368 ± 76 (75%) in OVCAR5 cells | |||
| 33391505 | 2021 | [125I]SST-scFv8D3 | 115 | 125I labeled | scFv of 8D3 is added to SST | Cyclic (Disulfide Bond Bw C-C Of SST) | L | Serine, threonine and glycine were added to the linker | Synthetic | Treatment of Alzheimer's diseases | Eight microliter blood samples from the tail vein were obtained at 0.5, 1, 2, 4, 6 and 24-h post injection | 0.44±0.08 MBq | 6 | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | The measured activation of neprilysin by SST-scFv8D3 preserved around 70% of the activation obtained by SST alone | |||
| 33387593 | 2021 | Wild-type (IFN) | 165 | Free | Free | Linear | L | None | Human derived | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 0.9 ± 0.1 (T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 201 ± 9 in wild-type IFN, Antiproliferative SBA (IU/ng) = 240 ± 50 | |||
| 33387593 | 2021 | GMOP-IFN | 179 | GM-CSF O-glycosylated Peptide | Free | Linear | L | None | Synthetic | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 3.0 ± 0.4(T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 190 ± 30 in GMOP-IFN, Antiproliferative SBA (IU/ng) = 280 ± 40 | |||
| 33387593 | 2021 | mGMOP-IFN | 180 | Modified GOMP | Free | Linear | L | None | Synthetic | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 2.5 ± 0.2 (T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 280 ± 50 in mGMOP-IFN, Antiproliferative SBA (IU/ng = 95 ± 5 | |||
| 33245951 | 2021 | GIP(1–42) | 42 | Free | Free | Linear | L | None | Secreted by entero-endocrine K cells located in the proximal intestine | Insulinotrophic Effect | Blood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min | 25 nmol/kg | 93 ± 2 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type= | None | N.A. | |||
| 33245951 | 2021 | GIP(1–42) | 42 | Free | Free | Linear | L | None | Secreted by entero-endocrine K cells located in the proximal intestine | Insulinotrophic Effect | Blood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min and then co-incubation with Val-Pyr | 25 nmol/kg | 5 ± 0.6 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type= | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 4.01 ± 1.19 | Human male blood protease | Two site ELISA | Human male blood sample | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 3.94 ± 1.10 | Human female blood protease | Two site ELISA | Human female blood sample | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 3.96 ± 1.12 | Human blood protease (All) | Two site ELISA | Human blood sample (All) | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33129837 | 2021 | OM19r-8 | 19 | Free | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Blood samples were collected in 1.5 mL capacity disposable tubes at 0.125, 0.25, 0.5, 0.75, 1, 5, 10, 15, 30, 45, 60 and 75min | 1 mg/ml | 1.632 ± 0.34 (Elimination Half Life) | Wistar rats blood protease | N.A. | Wistar rats blood sample | In Vivo | None | None | MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin | |||
| 33129837 | 2021 | mPEG5- OM19r-8 | 19 | mPEG5 | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Blood samples were collected in 1.5 mL capacity disposable tubes at 0.125, 0.25, 0.5, 0.75, 1, 5, 10, 15, 30, 45, 60 and 75min | 1 mg/ml | 28.09 ± 2.81 (Elimination Half Life) | Wistar rats blood protease | N.A. | Wistar rats blood sample | In Vivo | None | None | MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin | |||
| 33129837 | 2021 | OM19r-8 | 19 | Free | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Aliquots were analyzed after 0, 20, 30, 40, 60, 80, 90, 100, 120, 150, 180, 210, 240, 175 and 270min | 31.5 μmol/L | 71.10 ± 3.43 | Wistar rats blood plasma protease | HPLC | Wistar rats blood plasma | In Vitro | None | None | MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin | |||
| 33129837 | 2021 | mPEG5- OM19r-8 | 19 | mPEG5 | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Aliquots were analyzed after 0, 20, 30, 40, 60, 80, 90, 100, 120, 150, 180, 210, 240, 270, 300, 400, 600 and 1000min | 31.5 μmol/L | 242.44 ± 39.21 | Wistar rats blood plasma protease | HPLC | Wistar rats blood plasma | In Vitro | None | None | MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin | |||
| 33049303 | 2021 | GLP-GA3-GS-L3 | 94 | Free | Free | Linear | L | GLP-1 linked with GA3 through L3 linker, FITC labeled | Synthetic | Antidiabetes | 8 h at 4 ◦C | 50 μg | 36.3 ± 7.8 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50) | |||
| 33049303 | 2021 | GLPABD035-GS-L3 | 93 | Free | Free | Linear | L | GLP-1 linked with ABD035 through L3 linker, amino acid subsituitions with F,R,K,E,K,L,H, FITC labeled | Synthetic | Antidiabetes | 8 h at 4 ◦C | 50 μg | 31.3 ± 1.0 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50) | |||
| 33049303 | 2021 | GLP-ABDCon-GS-L3 | 93 | Free | Free | Linear | L | GLP-1 linked with ABDCon through L3 linker, amino acid subsituitions with K,E,K,I,E,K,I,T,F,D,K,N,K,K, FITC labeled | Synthetic | Antidiabetes | 8 h at 4 ◦C | 50 μg | 38.3 ± 2.7 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50) | |||
| 32778037 | 2021 | [14C]-WLBU2 | 24 | C14 labeling | Free | Linear | L | None | Synthetic | Antimicrobial | N.A. | 15 mg/kg | 22 (Radioactivity Half Life) | CD1 female mice plasma protease | Radiochromatography | CD1 female mice plasma | In Vivo | None | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | Conventional unsubstituted β-eliminative linker, linked by a GDM linker and Mod = (CH3)2NSO2− | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | ~2020 (Release Half Life) | N.A. | N.A. | N.A. | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | Conventional unsubstituted β-eliminative linker | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | 900 (Release Half Life) | Rats | N.A. | Rats | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | with GDM linker and Mod = (CH3)2NSO2− | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | ~1800 (Release Half Life) | N.A. | N.A. | N.A. | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | Conventional unsubstituted β-eliminative linker | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | 750 (Release Half Life) | Rats | N.A. | Rats | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 33801382 | 2021 | [177Lu]Lu-NeoB | 7 | Acetylation, 177Lu Labelling | Aminoethylamide -NH-CH(CH2-CH(CH3)2)2 | Linear | Mix | None | Derived from the antagonist GRPR peptide SB3 | Antitumor (Treatment of Gastrointestinal Stromal Tumors) | N.A. | N.A. | 40.2 (Distribution Half Life) | N.A. | N.A. | N.A. | N.A. | https://pmc.ncbi.nlm.nih.gov/articles/PMC6150197/ | None | [177Lu]Lu-NeoB tumor uptake in 400 pmol group mice (~11% ID/g) was found to be higher than that observed in 800 pmol group mice (~7% ID/g) |