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 |
| InChI | 1S/C25H30N4O2/c1-19-17-23(21-9-5-6-10-22(21)27-19)28-24(30)26-13-16-29-14-11-25(31,12-15-29)18-20-7-3-2-4-8-20/h2-10,17,31H,11-16,18H2,1H3,(H2,26,27,28,30) |
| InChIKey | WYJCYXOCHXWTHG-UHFFFAOYSA-N |
| SMILES | N3(CCC(CC3)(O)Cc4ccccc4)CCNC(=O)Nc1c2c(nc(c1)C)cccc2 |
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 |
| WGK Germany | WGK 3 |
| 存储类别 | 11 - Combustible Solids |
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 |
| 2026/09/15 | HY-10655R | ACT 058362; PALOSURAN, Palosuran (Standard) | 540769-28-6 | 1 mg | 800元 |
| 2026/09/15 | HY-10655R | ACT 058362; PALOSURAN, Palosuran (Standard) | 540769-28-6 | 5 mg | 2000元 |
| 2026/09/15 | HY-10655R | ACT 058362; PALOSURAN, Palosuran (Standard) | 540769-28-6 | 10 mg | 3250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). |
