For research use only. Not for therapeutic Use.
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].
Protease-Activated Receptor-1, PAR-1 Agonist induces activation of protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma cells expressing PAR1 endogeneously. On the cellular level, Protease-Activated Receptor-1, PAR-1 Agonist and thrombin prompted HT-29 cell migration and matrix adhesion by a PKCepsilon-dependent mechanism as concluded because of the inhibition of PAR1-mediated effects by the PKC inhibitor bisindolylmaleimide I and the PKCepsilon translocation inhibitory peptide EAVSLKPT but not by the PKC inhibitor Gö 6976[2].
| Catalog Number | I044270 |
| Synonyms | (2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-oxobutanoic acid;2,2,2-trifluoroacetic acid |
| Molecular Formula | C37H59F3N10O11 |
| Purity | ≥95% |
| InChI | InChI=1S/C35H58N10O9.C2HF3O2/c1-18(2)14-23(30(49)41-22(12-9-13-40-35(38)39)29(48)45-26(34(53)54)17-27(36)47)42-31(50)24(15-19(3)4)43-32(51)25(16-21-10-7-6-8-11-21)44-33(52)28(37)20(5)46;3-2(4,5)1(6)7/h6-8,10-11,18-20,22-26,28,46H,9,12-17,37H2,1-5H3,(H2,36,47)(H,41,49)(H,42,50)(H,43,51)(H,44,52)(H,45,48)(H,53,54)(H4,38,39,40);(H,6,7)/t20-,22+,23+,24+,25+,26+,28+;/m1./s1 |
| InChIKey | UBOKANGGJHPUIA-ZZWRYBPMSA-N |
| SMILES | CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(C(C)O)N.C(=O)(C(F)(F)F)O |
| Reference | [1]. Stefanie Gödecke, et al. Thrombin-induced ATP release from human umbilical vein endothelial cells. Am J Physiol Cell Physiol. 2012 Mar 15;302(6):C915-23. [2]. Heider I, et al. PAR1-type thrombin receptor stimulates migration and matrix adhesion of human colon carcinoma cells by a PKCepsilon-dependent mechanism. Oncol Res. 2004;14(10):475-482. |
