产品描述:
Vericiguat is a stimulator of soluble guanylyl cyclase (sGC).{62821} It stimulates the formation of cGMP in CHO cells expressing recombinant rat sGC in the absence and presence of the nitric oxide (NO) donor SNAP (Item No. 82250; EC50s = 1,005 and 39 nM, respectively), an effect that can be reversed by the sGC inhibitor ODQ (Item No. 81410). Vericiguat inhibits phenylephrine-induced contractions in isolated rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings (IC50s = 798, 692, and 3,072 nM, respectively), as well as decreases the coronary perfusion pressure in isolated perfused rat hearts in a concentration-dependent manner. It decreases proteinuria and increases survival in rats expressing mouse renin ((mRenR2)27), a transgenic model for hypertension, when administered at doses of 3 or 10 mg/kg. Formulations containing vericiguat have been used in the treatment of heart failure.