Palosuran

Palosuran is an antagonist of the urotensin II receptor (UTR, IC50s = 3.6 and 1,475 nM for CHO cell membranes expressing human and rat recombinant receptors, respectively). It inhibits contraction of isolated rat aortic rings induced by urotensin II (Cay-24711, Cay-24753) in a concentration-dependent manner. Palosuran (300 mg/kg twice per day) reduces plasma endothelin-1 (Cay-24127), urotensin II, and TGF-beta1 levels, as well as the main pulmonary arterial pressure and right ventricular hypertrophy index in a rat model of pulmonary arterial hypertension (PAH) induced by monocrotaline (Cay-16666). Palosuran (300 mg/kg per day) reduces serum glucose, cholesterol, and triglyceride levels and increases survival in a rat model of diabetes induced by streptozotocin (STZ, Cay-13104). It also decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats.Formal Name: N-[2-[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)-urea. CAS Number: 540769-28-6. Synonyms: ACT058362. Molecular Formula: C25H30N4O2. Formula Weight: 418.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 216, 234, 338 nm. SMILES: OC1(CCN(CCNC(NC2=CC(C)=NC3=C2C=CC=C3)=O)CC1)CC4=CC=CC=C4. InChi Code: InChI=1S/C25H30N4O2/c1-19-17-23(21-9-5-6-10-22(21)27-19)28-24(30)26-13-16-29-14-11-25(31,12-15-29)18-20-7-3-2-4-8-20/h2-10,17,31H,11-16,18H2,1H3,(H2,26,27,28,30). InChi Key: WYJCYXOCHXWTHG-UHFFFAOYSA-N.