Riociguat

Riociguat is a stimulator of soluble guanylate cyclase (sGC)., It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 µM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Cay-82100). It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 µM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Cay-16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.Formal Name: N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methyl-carbamic acid, methyl ester. CAS Number: 625115-55-1. Synonyms: BAY 63-2521. Molecular Formula: C20H19FN8O2. Formula Weight: 422.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml. lambdamax: 212, 323 nm. SMILES: FC1=C(CN2C(N=CC=C3)=C3C(C4=NC(N)=C(N(C)C(OC)=O)C(N)=N4)=N2)C=CC=C1. InChi Code: InChI=1S/C20H19FN8O2/c1-28(20(30)31-2)15-16(22)25-18(26-17(15)23)14-12-7-5-9-24-19(12)29(27-14)10-11-6-3-4-8-13(11)21/h3-9H,10H2,1-2H3,(H4,22,23,25,26). InChi Key: WXXSNCNJFUAIDG-UHFFFAOYSA-N.