Fulacimstat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Fulacimstat (BAY 1142524, BAY1142524) 是一种有效的口服食糜酶抑制剂，对人和仓鼠食糜酶的 IC50 分别为 4 nM 和 3 nM。

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; blocks the generation of profibrotic chymase-dependent factors such as Ang II, ET-1, and TGF-β1 in vitro with a nanomolar IC50; 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.?Other Indication Phase 2 Clinical(In Vitro):Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively.(In Vivo):Isoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation.

Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively.

Isoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation.

BAY 1142524 | BAY1142524 | BAY-1142524

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Other Disease

1488354-15-9

487.39

C23H16F3N3O6

>98% (HPLC)

DMSO : 5 mg/mL 10.26 mM

O=C(C1=CN(C2=CC=C3N(C)C(OC3=C2)=O)C(N([C@@H]4CCC5=C4C=CC=C5C(F)(F)F)C1=O)=O)O

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

(-20℃)

With Ice Pack

≥ 2 years