ACT 058362; PALOSURAN,
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) |
| 颜色 | 白至粉红 |
ACT 058362; PALOSURAN, 用途与合成方法
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). |
ACT 058362; PALOSURAN, 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-02-08 | HY-10655 | 540769-28-6 | 10 mM * 1 mLin DMSO | 866 | |
| 2025-02-08 | HY-10655 | ACT 058362; PALOSURAN, | 540769-28-6 | 5mg | 940 |
