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维利西呱 /Vericiguat {[allProObj[0].p_purity_real_show]}

货号:A664188 同义名: BAY1021189;Verquvo Ambeed 开学季,买赠积分,赢豪礼

Vericiguat targets soluble guanylate cyclase (sGC) and is used for treating heart failure.

Vericiguat 化学结构 CAS号:1350653-20-1
Vericiguat 化学结构
CAS号:1350653-20-1
Vericiguat 3D分子结构
CAS号:1350653-20-1
Vericiguat 化学结构 CAS号:1350653-20-1
Vericiguat 3D分子结构 CAS号:1350653-20-1
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Vericiguat 纯度/质量文件 产品仅供科研

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Vericiguat 生物活性

描述 Vericiguat enhances the activity of recombinant soluble guanylate cyclase (sGC) in a concentration-dependent manner, ranging from a 1.7-fold to a 57.6-fold increase. In combination with the nitric oxide donor diethylamine/nitric oxide complex (DEA/NO), Vericiguat and DEA/NO exhibit a synergistic effect on sGC activity across various concentrations. At the highest concentrations tested (100 μM for Vericiguat and 100 nM for DEA/NO), sGC activity is elevated 341.6-fold above the baseline. Vericiguat also concentration-dependently activates an sGC reporter cell line, with an EC50 of 1005±145 nM. It concentration-dependently inhibits phenylephrine-induced contractions in rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings, with IC50 values of 798, 692, and 3072 nM, respectively. Moreover, Vericiguat concentration-dependently inhibits U46619-induced contractions in porcine coronary artery rings, with an IC50 of 956 nM[1].
体内研究

With oral administration at doses of 3 mg/kg and 10 mg/kg once daily for 21 days, Vericiguat preserves heart and kidney function in a model of hypertension-induced end-organ damage in L-NAME-treated renin transgenic rats. Importantly, the Vericiguat-treated group exhibits a significant reduction in overall mortality compared to the control group[1].

体外研究

Vericiguat enhances the activity of recombinant soluble guanylate cyclase (sGC) in a concentration-dependent manner, ranging from a 1.7-fold to a 57.6-fold increase. In combination with the nitric oxide donor diethylamine/nitric oxide complex (DEA/NO), Vericiguat and DEA/NO exhibit a synergistic effect on sGC activity across various concentrations. At the highest concentrations tested (100 μM for Vericiguat and 100 nM for DEA/NO), sGC activity is elevated 341.6-fold above the baseline. Vericiguat also concentration-dependently activates an sGC reporter cell line, with an EC50 of 1005±145 nM. It concentration-dependently inhibits phenylephrine-induced contractions in rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings, with IC50 values of 798, 692, and 3072 nM, respectively. Moreover, Vericiguat concentration-dependently inhibits U46619-induced contractions in porcine coronary artery rings, with an IC50 of 956 nM[1].

Vericiguat 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.

Vericiguat 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.73mL

2.35mL

1.17mL

23.45mL

4.69mL

2.35mL

Vericiguat 技术信息

CAS号1350653-20-1
分子式C19H16F2N8O2
分子量 426.38
别名 BAY1021189;Verquvo
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 60 mg/mL(140.72 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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