
Fulacimstat
CAS No. 1488354-15-9
Fulacimstat ( BAY 1142524 | BAY1142524 | BAY-1142524 )
产品货号. M12057 CAS No. 1488354-15-9
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。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥2341 | 有现货 |
![]() ![]() |
10MG | ¥3345 | 有现货 |
![]() ![]() |
25MG | ¥5605 | 有现货 |
![]() ![]() |
50MG | ¥7979 | 有现货 |
![]() ![]() |
100MG | ¥10773 | 有现货 |
![]() ![]() |
200MG | 获取报价 | 有现货 |
![]() ![]() |
500MG | 获取报价 | 有现货 |
![]() ![]() |
1G | 获取报价 | 有现货 |
![]() ![]() |
生物学信息
-
产品名称Fulacimstat
-
注意事项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
-
产品简述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。
-
产品描述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.
-
体外实验Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively.
-
体内实验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.
-
同义词BAY 1142524 | BAY1142524 | BAY-1142524
-
通路Others
-
靶点Other Targets
-
受体Other Targets
-
研究领域Other Indications
-
适应症Other Disease
化学信息
-
CAS Number1488354-15-9
-
分子量487.39
-
分子式C23H16F3N3O6
-
纯度>98% (HPLC)
-
溶解度DMSO : 5 mg/mL 10.26 mM
-
SMILESO=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
-
化学全称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
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
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.
产品手册




关联产品
-
Sitafloxacin Hydrate
西他沙星(INN;也称为 DU-6859a)是一种氟喹诺酮类抗生素,在治疗布鲁里溃疡方面显示出良好的前景。
-
3',4',5',5,7-Pentame...
3',4',5',5,7-Pentamethoxyflavanone 是一种天然黄酮化合物,在 Neoraptua magnifica var. magnifica 中发现。
-
Orexin A (human, rat...
Endogenous agonist at orexin receptors (Ki values are 20 and 38 nM for OX1 and OX2 receptors respectively). Stimulates feeding following central administration and may be involved in the control of sleep-wake cycle and other hypothalamic functions.