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Chemical Structure : BR103354
CAS No.: 2505339-87-5
Catalog No.: PC-72073Not For Human Use, Lab Use Only.
BR103354 (BR 103354) is a novel potent, selective, oral fibroblast activation protein (FAP) inhibitor with IC50 of 14 nM.
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BR103354 (BR 103354) is a novel potent, selective, oral fibroblast activation protein (FAP) inhibitor with IC50 of 14 nM.
BR103354 displays high selectivity against other related proteases with a selectivity index (SI) of 27.6 against PREP (PREP IC50=387 nM).
BR103354 (0.4 uM) blocked FAP-mediated cleavage of hFGF21 in cell-free assays; In differentiated 3T3/L1 adipocytes, the addition of FAP diminished hFGF21-induced Glut1 and phosphorylated levels of ERK, which were restored by BR103354.
BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition.
BR103354 reduced nonfasting blood glucose concentrations with improved glucose tolerance and with reduced triglyceride (TG) content in liver of ob/ob mice, improved hepatic steatosis and fibrosis in NASH mouse model.
| M.Wt | 415.419 | |
| Formula | C19H15F2N5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (4.15 mg/mL) |
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| Chemical Name/SMILES |
(S)-N-(2-(2-Cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)-2-(4-cyanobenzyl)thiazole-4-carboxamide |
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1. Jae Min Cho, et al. Sci Rep. 2020 Dec 4;10(1):21280.
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