255913-18-9

Upstream product

• 78981-73-4 Boc-p-F-Phe-NH₂ 
• 212756-39-3 2-[1-[2-(tert-butoxycarbonyl-methyl-amino)-acetylamino]-2-(4-fluoro-phenyl)-ethyl]-thiazole-4-carboxylic acid ethyl ester 
• 212756-38-2 Ethyl 2-[1(S)-t-butoxycarbonylamino-2-(4-fluorophenyl)ethyl]thiazole-4-carboxylate 
• 255913-22-5 [2-(4-fluoro-phenyl)-1-thiocarbamoyl-ethyl]-carbamic acid tert-butyl ester 
• 212756-40-6 (S)-2-({2-[(S)-1-[2-(tert-Butoxycarbonyl-methyl-amino)-acetylamino]-2-(4-fluoro-phenyl)-ethyl]-thiazole-4-carbonyl}-amino)-3-cyclohexyl-propionic acid methyl ester 

Relevant academic research and scientific papers

Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif

The thrombin receptor (PAR-1) is activated by α-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. A series of azole-based carboxamides, designed after SFLLR, were synthesized and evaluated in vitro. The compounds inhibited platelet aggregation induced by SFLLRN-NH2 or α-thrombin, and blocked the binding of [3H]-S-(p-F-Phe)-Har-L-Har-KY-NH2 to a CHRF membrane preparation of PAR-1. Oxazole 30 bound to PAR-1 with an IC50 of 1.6 μM, and gave IC50 values of 25 μM and 6.6 μM against α-thrombin- and SFLLRN-NH2-induced platelet aggregation, respectively.