维利西呱 T17226

Product Introduction
Bioactivity


英文名: Vericiguat

描述: Vericiguat (BAY1021189) 是一种有效的口服鸟苷酸环化酶刺激剂。

体外活性: Vericiguat inhibits the U46619-induced contractions of porcine coronary artery rings concentration-dependently (IC50: 956 nM). Vericiguat inhibits phenylephrine-induced contractions of rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings concentration-dependently (IC50: 798, 692, and 3072 nM, respectively). 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, Vericiguat and DEA/NO have a synergistic effect on the enzyme activity over a wide range of concentrations. At the 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 (EC50: 1005±145 nM) [1].

体内活性: Vericiguat causes a significant and dose-dependent increase in survival rates. Chronic oral treatment with Vericiguat (3 or 10 mg/kg, q.d.) results in a significant attenuation of blood pressure increase during the course of the study. Vericiguat (3 or 10 mg/kg) treatment leads to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction. In the 3 and 10 mg/kg q.d. treatment groups, the rat survival rate is 70% and 90%, respectively, at the study end [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (105.54 mM)


关键字: Inhibitor | Vericiguat | inhibit | BAY 1021189 | Guanylate Cyclase | BAY-1021189

相关产品: Nitroprusside disodium dihydrate | Sinitrodil | Guanylin (mouse, rat) | Lificiguat | Glutaminyl Cyclase Inhibitor 1 | NS-2028 | Indusatumab | ODQ | Uroguanylin (human) | Plecanatide

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途