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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Dipeptidyl Peptidase (DPP)-BR103354
BR103354

Chemical Structure : BR103354

CAS No.: 2505339-87-5

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BR103354 (BR 103354)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 415.419
分子式 C19H15F2N5O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (4.15 mg/mL)
Chemical Name/SMILES

(S)-N-(2-(2-Cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)-2-(4-cyanobenzyl)thiazole-4-carboxamide

参考文献

1. Jae Min Cho, et al. Sci Rep. 2020 Dec 4;10(1):21280.

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