An antagonist of UTR (IC50s = 3.6 and 1

Palosuran – 10 mg

Brand:
Cayman
CAS:
540769-28-6
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An antagonist of UTR (IC50s = 3.6 and 1,475 nM for CHO cell membranes expressing human and rat recombinant receptors, respectively); inhibits urotensin II-induced contraction of isolated rat aortic rings in a concentration-dependent manner; reduces plasma endothelin-1, urotensin II, and TGF-β1 levels, as well the main pulmonary arterial pressure and right ventricular hypertrophy index in a monocrotaline-induced rat model of PAH at 300 mg/kg twice per day; reduces serum glucose, cholesterol, and triglyceride levels and increases survival in an STZ-induced rat model of diabetes at 300 mg/kg per day; 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

Synonyms:  ACT058362

Molecular weight: 418.5

CAS: 540769-28-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Lipids & Lipoproteins||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias

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