PRX-08066

PRX-08066 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B. It binds to 5-HT2B receptors (Ki = 3.4 nM) and inhibits 5-HT-induced MAPK activation and thymidine incorporation in CHO cells expressing human 5-HT2B (IC50s = ~12 and ~3 nM, respectively). PRX-08066 (50 and 100 mg/kg) reduces peak pulmonary arterial pressure and right ventricular hypertrophy in a rat model of pulmonary hypertension induced by monocrotaline (MCT, Cay-16666).Formal Name: 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-benzonitrile. CAS Number: 866206-54-4. Molecular Formula: C19H17ClFN5S. Formula Weight: 401.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 96mg/ml, Ethanol: 91 mg/ml, Water: 95 mg/ml. lambdamax: 221, 279 nm. SMILES: ClC1=CC(C(S1)=NC=N2)=C2NC3CCN(CC3)CC4=CC(C#N)=C(C=C4)F. InChi Code: InChI=1S/C19H17ClFN5S/c20-17-8-15-18(23-11-24-19(15)27-17)25-14-3-5-26(6-4-14)10-12-1-2-16(21)13(7-12)9-22/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25). InChi Key: IENZFHBNCRQMNP-UHFFFAOYSA-N.