Palosuran
| CAS号 | 540769-28-6 | 货号 | BCP15786 |
| 中文名 | Palosuran | ||
| 英文名 | Palosuran | ||
| 中文别名 | |||
| 英文别名 | ACT-058362;ACT 058362;ACT058362; | ||
| 分子式 | C25H30N4O2 | 分子量 | 418.53 |
| 生物活性 | Palosuran inhibited 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors almost as potently as cold U-II, with an IC50 of 3.6 ± 0.2 nM. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells). Compared with the human UT receptor, the binding inhibitory potency of palosuran against the rat UT receptor was lower in membrane preparation (400-fold), as well as in cells (>120-fold) . in vivo: Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. Furthermore, palosuran increased renal blood flow and delayed the development of proteinuria and renal damage . Palosuran was rapidly absorbed with maximum plasma concentrations at 1 hour after drug administration. The accumula | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | Urotensin Receptor | ||
结构式
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