公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)!

抑制剂描述:

产品名称:Vericiguat

产品别名:见爱必信官网

英文别名:Vericiguat

靶点:Guanylate Cyclase

CAS:1350653-20-1

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Vericiguat (BAY1021189) 是一种有效的、可溶的鸟苷酸环化酶 (guanylate cyclase) 抑制剂。

溶解性:DMSO : 60 mg/mL (140.72 mM; Need ultrasonic)

体外研究:

Vericiguat (0.01 μM to 100 μM) stimulates recombinant sGC concentration dependently, by 1.7-fold to 57.6-fold. When combined with the NO donor diethylamine/nitric oxide complex (DEA/NO), vericiguat and DEA/NO have a synergistic effect on the enzyme activity over a wide range of concentrations. At highest concentrations of vericiguat (100 μM) and DEA/NO (100 nM), the specific activity of sGC is 341.6-fold above baseline. Vericiguat stimulates the sGC reporter cell line concentration dependently, with an EC50 of 1005±145 nM. Vericiguat inhibits phenylephrine-induced contractions of rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings concentration dependently, with IC50 values of 798, 692, and 3072 nM, respectively. Vericiguat inhibits the U46619-induced contractions of porcine coronary artery rings concentration dependently, with an IC50 of 956 nM.

体内研究:Chronic oral treatment with 3 or 10 mg/kg vericiguat qd results in a significant attenuation of blood pressure increase during the course of the study. However, the overall rise of blood pressure increase is not halted in the 3 and 10 mg/kg treatment groups. Vericiguat treatment at 3 or 10 mg/kg leads to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction. Vericiguat results in a significant and dose-dependent increase in survival rates. In the 3 and 10 mg/kg qd treatment groups, the rat survival rate is 70% and 90%, respectively, at the study end.

产品信息订购:

产品更多信息请进入爱必信网站咨询