生物活性 | |||
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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 | |||
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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 |
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