Palosuran hydrochloride (ACT-058362 hydrochloride) 是一种有效，选择性和具有口服活性的urotensin II receptor受体拮抗剂，对于表达人重组受体的 CHO 细胞膜的IC50值为 3.6 nM。Palosuran hydrochloride 可改善糖尿病大鼠的胰腺和肾脏功能。

Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC 50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats [1] [2].

Palosuran (8 h) inhibits 125 I-U-II binding to human UT receptor, with IC 50 s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells [1]. Palosuran inhibits Ca 2+ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC 50 s of 17 and >10000 nM, respectively [1]. Palosuran (0.12-10000 nM; 20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells, with an IC 50 of 150 nM [1].

ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure [1]. Palosuran (300 mg/kg/d; p.o. for 16 weeks) improves the survival, increases insulin, and slows the increase in glycemia, glycosylated hemoglobin, and serum lipids in streptozotocin-induced diabetic rats [2]. Animal Model: Male Wistar rats with renal ischemia and reperfusion [1] Dosage: 20 mg/kg/h for 135 min Administration: I.v. (continuous infusion) for 135 min Result: Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values. Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR).

2469274-58-4

C25H31ClN4O2

454.99

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years