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Vericiguat

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Chemical Structure| 1350653-20-1 同义名 : BAY1021189;Verquvo
CAS号 : 1350653-20-1
货号 : A664188
分子式 : C19H16F2N8O2
纯度 : 99%+
分子量 : 426.38
MDL号 : MFCD28502029
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:
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].
实验方案
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

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.