Formulation: A crystalline solid
Formal Name: N-[2-[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)-urea
Purity: ≥98%
Formula Markup: C25H30N4O2
Formula Weight: 418,5
Shelf life (days): 1460
CAS Number: 540769-28-6
Notes: 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).{47224} It inhibits contraction of isolated rat aortic rings induced by urotensin II (Item Nos. 24711 / 24753) in a concentration-dependent manner. Palosuran (300 mg/kg twice per day) reduces plasma endothelin-1 (Item No. 24127), urotensin II, and TGF-β1 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 (Item No. 16666).{47225} 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; Item No. 13104).{47226} It also decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats.
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