Nelociguat

Nelociguat is a stimulator of soluble guanylate cyclase (sGC) and an active metabolite of riociguat (Cay-9000554). It is formed from riociguat by the cytochrome P450 (CYP) isoform CYP1A1. Nelociguat increases phosphorylation of the protein kinase G (PKG) substrate vasodilator-stimulator protein (VASP) in isolated rat aortic smooth muscle cells (EC50 = 353 nM). It induces vasodilation in rat aortic rings (EC50 = 75 nM). Nelociguat (3 mg/kg) decreases urine output and cardiac hypertrophy, as well as improves survival, in spontaneously hypertensive stroke-prone rats fed a high-salt high-fat diet. It improves erectile responses to electrical stimulation of the cavernous nerve in a rat model of cavernous nerve crush injury when administered at doses of 0.03 and 0.3 mg/kg.Formal Name: N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-carbamic acid, methyl ester. CAS Number: 625115-52-8. Synonyms: BAY 60-4552, Desmethyl Riociguat. Molecular Formula: C19H17FN8O2. Formula Weight: 408.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: slightly, heated, Methanol: very slightly, heated. SMILES: O=C(NC1=C(N)N=C(C2=NN(CC3=C(F)C=CC=C3)C4=C2C=CC=N4)N=C1N)OC. InChi Code: InChI=1S/C19H17FN8O2/c1-30-19(29)24-14-15(21)25-17(26-16(14)22)13-11-6-4-8-23-18(11)28(27-13)9-10-5-2-3-7-12(10)20/h2-8H,9H2,1H3,(H,24,29)(H4,21,22,25,26). InChi Key: FTQHGWIXJSSWOY-UHFFFAOYSA-N.