Vericiguat

Vericiguat is a stimulator of soluble guanylyl cyclase (sGC). 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 (Cay-82250, EC50s = 1,005 and 39 nM, respectively), an effect that can be reversed by the sGC inhibitor ODQ (Cay-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.Formal Name: N-[4,6-diamino-2-[5-fluoro-1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-carbamic acid, methyl ester. CAS Number: 1350653-20-1. Synonyms: BAY-1021189, MK-1242. Molecular Formula: C19H16F2N8O2. Formula Weight: 426.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, Ethanol: insol, PBS (pH 7.2): insol. lambdamax: 257 nm. SMILES: O=C(NC1=C(N)N=C(C2=NN(CC3=C(F)C=CC=C3)C4=C2C=C(F)C=N4)N=C1N)OC. InChi Code: InChI=1S/C19H16F2N8O2/c1-31-19(30)25-14-15(22)26-17(27-16(14)23)13-11-6-10(20)7-24-18(11)29(28-13)8-9-4-2-3-5-12(9)21/h2-7H,8H2,1H3,(H,25,30)(H4,22,23,26,27). InChi Key: QZFHIXARHDBPBY-UHFFFAOYSA-N.