540769-28-6
540769-28-6 結(jié)構(gòu)式
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)-
物理化學性質(zhì)
常見問題列表
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). |