| 1002 | Cyclosporin A (CsA) | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungus | Reduction of the IL-2 surface receptor CD25 expression (76%±11 after 24 hrs and 62%±7.3 after 36 hrs), also reduces TNF-α expression (23%±1.8) | Inhibits the production of IL-2 | In vitro | Human peripheral Lymphocytes and purified T cells | NA | None | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1036 | Cyclosporin A | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | From fungus Trichoderma polysporum | Inhibit IL-2 production by activated CD4+ T-cells | Inhibiting the calcineurin pathway | Both | Peripheral blood mononuclear cells (PBMCs) | 61.8 nM for CD4+ T cell activation of IL-2 production | C57/B6 mice | MIC assay, Immunosuppression and toxicity test | NA | NA | 18599825 | 2008 |
| 1044 | Cyclosporin A | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | From fungus Trichoderma polysporum | Ca2+-dependent permeability transition | Inhibit the Ca2+ dependent permeability transition | In vivo | NA | NA | Male Sprague-Dawley rat | NA | NA | NA | 2470734 | 1989 |
| 1089 | Cyclosporin A (CyA) | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungi | IL-1, IL-8, TNF-α | Inhibits the expression of cytokine genes; lower the activity of T cells and their immune response | In vitro | Murine KC line PAM 212,human squamous carcinoma line COLO-16 | 4.5micromolar | NA | Thymocyte co-stimulator assay | NA | NA | 8148271 | 1994 |
| 1090 | Cyclosporin A (CyA) | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungi | IL-1, lL-8, TNF-α | Inhibits the expression of cytokine genes; lower the activity of T cells and their immune response | In vitro | Normal human KCs | 2micromolar | NA | Thymocyte co-stimulator assay | NA | NA | 8148271 | 1994 |
| 1113 | Cyclosporin A | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Tolypocladium inflatum (fungus) | Calcineurin | Inhibition of calcineurin by complex with cyclophilins | Both | Murine KC line PAM 212,human squamous carcinoma line COLO-16 | NA | Sprague Dawley rats | NA | NA | NA | 24333193 | 2014 |
| 1139 | Cyclosporin A (CsA) | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungus | NA | Inhibits virus-induced polykaryocyte formation and the production of infectious measles virus | In vitro | Vero cells (Persistently infected Vero cells (448-PI-Vero)) | 5micromolar | NA | NA | NA | NA | 11509881 | 2001 |
| 1145 | Cyclosporin A (CsA) | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungus | NA | Not Available | In vivo | NA | NA | Eight- to 12-week-old male Lewis.lW (RTI.u) and Lewis.lA (RTI.')rats | Graft transplation assay | NA | NA | 10666482 | 2000 |
| 1173 | Cyclosporin A | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungus | NA | Not Available | In vivo | NA | NA | CBA/Ca and (CBA/Ca X C57BL6)F1 mice | Plaque-forming cell (PFC) assay | NA | NA | 6159410 | 1980 |
| 1341 | Formula 3 | R-Sar-DV | 4 | L | None | None | Sar = N-Methylglycine (aka sarcosine) | Linear | Synthetic | NA | Suppress the antigen presentation of macrophages or antigen recognition of T-cells in the immune processes | Inhibit maturation of the T-cell dependent antibody producing cells, supress the phagocytosis and dminish the late hypersensitive response | In vitro | Splenocyte s obtained from rats | NA | Twelve Wistar (LATI) rats | Hummoral Immune Response assay | NA | NA | US 5093320 | 1992 |
| 1342 | Formula 4 | R-Sar-D | 3 | L | None | None | Sar = N-Methylglycine (aka sarcosine) | Linear | Synthetic | NA | Suppress the antigen presentation of macrophages or antigen recognition of T-cells in the immune processes | Inhibit maturation of the T-cell dependent antibody producing cells, supress the phagocytosis and dminish the late hypersensitive response | In vitro | Splenocyte s obtained from rats | NA | Twelve Wistar (LATI) rats | Hummoral Immune Response assay | NA | NA | US 5093320 | 1992 |
