540769-28-6

基本信息
ACT 058362
PALOSURAN,, >98%
ACT058362
ACT-058362
ACT 058362
PALOSURAN,
ACT 058362
PALOSURAN,, >98%
1-[2-(4-Benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
N-[2-[4-Hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)urea
Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-
物理化学性质
沸点 | 612.9±55.0 °C(Predicted) |
密度 | 1.235±0.06 g/cm3(Predicted) |
储存条件 | -20°C储存 |
溶解度 | DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 0.5 mg/ml |
酸度系数(pKa) | 12.95±0.43(Predicted) |
形态 | 结晶固体 |
颜色 | White to pink |
安全数据
危险性符号(GHS) | ![]() GHS07 |
警示词 | 警告 |
危险性描述 | H302-H315-H320-H335 |
防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
ACT 058362; PALOSURAN,价格(试剂级)
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2025/02/08 | HY-10655 | Palosuran | 540769-28-6 | 10 mM * 1 mLin DMSO | 866元 |
2025/02/08 | HY-10655 | ACT 058362; PALOSURAN, Palosuran | 540769-28-6 | 5mg | 940元 |
2025/02/08 | HY-10655 | ACT 058362; PALOSURAN, Palosuran | 540769-28-6 | 10mg | 1520元 |
常见问题列表
IC50: 3.6 nM (human urotensin II receptor)
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.
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). |