ACT 058362; PALOSURAN,
| 中文名称 | ACT 058362; PALOSURAN, |
|---|---|
| 中文同义词 | 化合物PALOSURAN |
| 英文名称 | Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)- |
| 英文同义词 | Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-;Palosuran;ACT 058362;ACT 058362; PALOSURAN,;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;ACT058362;ACT-058362;ACT 058362; PALOSURAN,, >98% |
| CAS号 | 540769-28-6 |
| 分子式 | C25H30N4O2 |
| 分子量 | 418.53 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | 540769-28-6.mol |
| 结构式 |  |
ACT 058362; PALOSURAN, 性质
| 沸点 | 612.9±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.235±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：10 mg/ml； DMSO：10 mg/ml； DMSO:PBS (pH 7.2) (1:1)：0.5 mg/ml；乙醇：0.5 mg/ml |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 12.95±0.43(Predicted) |
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). |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-10655 | Palosuran | 1 mg | 930元 | |
| 2024/04/30 | HY-10655 | ACT 058362; PALOSURAN, Palosuran | 540769-28-6 | 5mg | 2325元 |