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首页-小分子抑制剂&激动剂-Others-Other Targets-Fulacimstat
Fulacimstat

Chemical Structure : Fulacimstat

CAS No.: 1488354-15-9

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Fulacimstat (BAY 1142524, BAY1142524, BAY-1142524)

货号: PC-60514Not For Human Use, Lab Use Only.

Fulacimstat (BAY 1142524, BAY1142524) is a potent, orally available chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.

规格 价格 库存 数量
5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Fulacimstat (BAY 1142524, BAY1142524) is a potent, orally available chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.
Fulacimstat (BAY 1142524) blocks the generation of profibrotic chymase-dependent factors such as Ang II, ET-1, and TGF-β1 in vitro with a nanomolar IC50.
Fulacimstat (BAY 1142524) reduces isoprenaline-induced cardiac fibrosis and attenuates the deterioration of heart function after MI, increases left-ventricular ejection fraction in dogs with LVD induced by intracoronary microembolization with no effects on blood pressure or heart rate. 

物理化学性质&存储条件

分子量 487.39
分子式 C23H16F3N3O6
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
Chemical Name/SMILES

1-(3-methyl-2-oxo-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]pyrimidine-5-carboxylic acid

参考文献

1. Kanefendt F, et al. Clin Pharmacol Drug Dev. 2018 Jun 7. doi: 10.1002/cpdd.579.

2. Hanna Tinel, et al. Abstract 13624: A Novel Chymase Inhibitor BAY 1142524 Reduces Fibrosis and Improves Cardiac Function After Myocardial Infarction in Hamster. Circulation. 2017;136:A13624.

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