S82942-10mg Vericiguat 1350653-20-1 98% 10mg 1280.00 现货

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商品详情

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产品描述： Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
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： Vericiguat (compound 24) (oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days) maintains heart and kidney function in a model of hypertension-induced end-organ damage in L-NAME-treated renin transgenic rats. Additionally,Vericiguat-treated group substantially reduces overall mortality when compared to the control group. Animal Model: L-NAME-treated renin transgenic rats Dosage: 3 mg/kg, 10 mg/kg Administration: Oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days Result: Resulted in a significant attenuation of blood pressure increase, however the overall rise of blood pressure increase was not halted in the 3/10 mg/kg treatment groups.Resulted a significant and dose-dependent reduction of heart hypertrophy, in both the right and left ventricle.With respect to kidney damage, Vericiguat Led to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction.Resulted in a significant and dose-dependent increase in survival rates. The rat survival rate was 70% and 90%, respectively in the 3 and 10 mg/kg qd treatment groups. In contrast, the survival rate in the placebo group was only 25% after 21 days.
参考文献：
1. Follmann M, et al. Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. J Med Chem. 2017 Jun 22;60(12):5146-5161.
溶解性： Soluble in DMSO
保存条件： -20℃
配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.345 ml	11.727 ml	23.453 ml
5 mM	0.469 ml	2.345 ml	4.691 ml
10 mM	0.235 ml	1.173 ml	2.345 ml
50 mM	0.047 ml	0.235 ml	0.469 ml

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