Palosuran hydrochloride|2469274-58-4|(ACT-058362 hydrochloride)-陌孚医药/Medlife

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Palosuran hydrochloride (Synonyms: ACT-058362 hydrochloride)

目录号: PL12509 纯度: ≥98%

CAS No. :2469274-58-4

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中文名称	Palosuran hydrochloride
英文名称	Palosuran hydrochloride
英文别名	Palosuran hydrochloride;1-[2-(4-Benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea;hydrochloride
Cas No.	2469274-58-4
分子式	C₂₅H₃₁ClN₄O₂
分子量	454.99
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	IC50: 3.6 nM (human urotensin II receptor)
体外研究(In Vitro)	Palosuran (8 h) inhibits I-U-II binding to human UT receptor, with IC50s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells. Palosuran inhibits Ca mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC50s of 17 and >10000 nM, respectively. 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 IC50 of 150 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Clozel M, et, al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin [2]. Clozel M, et, al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21.

溶解度数据	In Vitro: DMSO : 50 mg/mL (109.89 mM; Need ultrasonic)H₂O : 7.14 mg/mL (15.69 mM; Need ultrasonic)配制储备液

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