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Details of TopicalPdb ID 1007

PRIMARY INFORMATION
ID1007
PMID24842663
Year2014
SequenceAAPV
NameC8(L)-Laa-AAPV
Length4
N-Terminal ModificationFree
C-Terminal ModificationFree
Linear/ CyclicLinear
ChiralityL
Chemical ModificationNone
Origin of PeptideSynthetic
Nature of Peptide/CargoIt fits the P-P1 subsites of elastase and inhibits HNE competitively
MechanismIncreased lipophilicity enhances permeation, enantiomeric selectivity is apparent
Cargo Sequence/StructureNone
Name of cargo
Not applicable
AssayFranz diffusion cell, HPLC
Enhancershort chain lipoamino acids (Laa: C8)
Properties of enhancerα-amino acids with a hydrocarbon side chain enhances permeability
Concentration2 mg in 200 μL of propylene glycol
Incubation time24 hours
Tissue permeability (value with units)Epidermal flux=1.37 μg/cm2/h, Permeability coefficient=4.50×10−4 Kp(cm/h)
Tissue SampleHuman epidermal membranes were obtained by heat separation of whole skin
Ex vivo/In vivo/In vitroin vitro
SECONDARY INFORMATION
STRUCTURE
Predicted Structure
SMILESN[C@@H](C)C(=O)N[C@@H](C)C(=O)N1C
CC[C@H]1C(=O)N[C@@H](C(C)C)C=O