ACT 058362; PALOSURAN,
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- CAS号:
- 540769-28-6
- 英文名:
- Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-
- 英文别名:
- Palosuran;ACT 058362;PALOSURAN,, >98%;ACT058362;ACT-058362;Palosuran (ACT058362);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)-
- 中文名:
- ACT 058362; PALOSURAN,
- 中文别名:
- 化合物PALOSURAN
- CBNumber:
- CB42628509
- 分子式:
- C25H30N4O2
- 分子量:
- 418.53
- MOL File:
- 540769-28-6.mol
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ACT 058362; PALOSURAN,化学性质
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沸点:
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612.9±55.0 °C(Predicted)
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密度:
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1.235±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 0.5 mg/ml
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形态:
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A crystalline solid
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酸度系数(pKa):
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12.95±0.43(Predicted)
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ACT 058362; PALOSURAN,性质、用途与生产工艺
Palosuran (ACT-058362) 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 可改善糖尿病大鼠的胰腺和肾脏功能。
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.
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Animal Model:
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Male Wistar rats with renal ischemia and reperfusion
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Dosage:
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20 mg/kg/h for 135 min
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Administration:
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I.v. (continuous infusion) for 135 min
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Result:
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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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ACT 058362; PALOSURAN,
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-10655 | Palosuran | | 1 mg | 930元 |
| 2024/01/25 | HY-10655 | ACT 058362; PALOSURAN,
Palosuran | 540769-28-6 | 5mg | 2325元 |
ACT 058362; PALOSURAN,
生产厂家
540769-28-6, ACT 058362; PALOSURAN, 相关搜索:
- Inhibitors
- 小分子抑制剂，天然产物
- 小分子抑制剂
- 化合物PALOSURAN
- 540769-28-6
- ACT058362,urotensin,Palosuran,Inhibitor,ischemia,diabetic,UT receptor,reperfusion,Urotensin Receptor,ACT 058362,renal,inhibit,pancreatic
- Palosuran (ACT058362)
- PALOSURAN,, >98%
- ACT 058362; PALOSURAN,, >98%
- ACT058362;ACT-058362
- N-[2-[4-Hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)urea
- 1-[2-(4-Benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
- ACT 058362; PALOSURAN,
- ACT 058362
- Palosuran
- Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-