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2469274-58-4

中文名称 化合物 PALOSURAN HYDROCHLORIDE
英文名称 Palosuran hydrochloride
CAS 2469274-58-4
分子式 C25H31ClN4O2
分子量 455
MOL 文件 2469274-58-4.mol
2469274-58-4 结构式 2469274-58-4 结构式

基本信息

英文别名
Palosuran hydrochloride

物理化学性质

储存条件-20°C储存
溶解度DMSO: 50 mg/mL (109.89 mM)
形态Solid
颜色White to off-white
水溶解性Water: 7.14 mg/mL (15.69 mM)
化合物 PALOSURAN HYDROCHLORIDE价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2026/09/15HY-10655A化合物 PALOSURAN HYDROCHLORIDE
Palosuran hydrochloride
2469274-58-45mg720元
2026/09/15HY-10655A化合物 PALOSURAN HYDROCHLORIDE
Palosuran hydrochloride
2469274-58-410mg1350元
2025/12/22HY-10655A化合物 PALOSURAN HYDROCHLORIDE
Palosuran hydrochloride
2469274-58-410mM * 1mLin DMSO721元

常见问题列表

生物活性
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。
靶点

IC50: 3.6 nM (human urotensin II receptor)

体外研究

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.
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.
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.

体内研究

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.

Animal Model: Male Wistar rats with renal ischemia and reperfusion
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).
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