貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S85687-5mg	99.4%	￥1600.00 S85687-5mg ￥1600.00 現(xiàn)貨	3 3	-	-	-
S85687-10mg	99.4%	￥2500.00 S85687-10mg ￥2500.00 現(xiàn)貨	8 8	-	-	-
S85687-50mg	99.4%	￥6500.00 S85687-50mg ￥6500.00 現(xiàn)貨	8 8	-	-	-

產(chǎn)品介紹

Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats

產(chǎn)品描述：

靶點(diǎn)：

IC50: 3.6 nM (human urotensin II receptor);GPR

體外研究：

Palosuran (8 h) inhibits 125I-U-II binding to human UT receptor, with IC50s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells. Palosuran inhibits Ca2+ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC50s 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 IC50 of 150 nM

體內(nèi)研究：

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).

參考文獻(xiàn)：

1. Clozel M, et al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System. J Pharmacol Exp Ther. 2004 Oct;311(1):204-12. 2. Clozel M, et al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.389 ml	11.947 ml	23.893 ml
5 mM	0.478 ml	2.389 ml	4.779 ml
10 mM	0.239 ml	1.195 ml	2.389 ml
50 mM	0.048 ml	0.239 ml	0.478 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

質(zhì)檢證書(COA)

輸入產(chǎn)品批號(hào)：

如何獲取質(zhì)檢證書(COA)?

請(qǐng)輸入貨號(hào)和一個(gè)與之匹配的批號(hào)。
例如:
批號(hào)：JS298415 貨號(hào)：S20001-25g
在貨品標(biāo)簽上如何找到貨號(hào)和批號(hào)?

摩爾濃度計(jì)算器

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

質(zhì)量

濃度

體積

分子摩爾量

計(jì)算重置

玖玖资源网站,爆乳久久久,日韩精品乱码久久久蜜桃,精品呦国产一区二区三区,国产伦高清一区二区三区,sese一区二区,午夜精品福利一区二区三区,三级黄色网站久久免费