VUF10460

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Chemical Structure| 1028327-66-3 同义名 : -
CAS号 : 1028327-66-3
货号 : A104244
分子式 : C15H19N5
纯度 : 99%+
分子量 : 269.34
MDL号 : MFCD13187037
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Histamine H4 receptor expression was detected by immunohistochemistry in different areas of the gut and protective effects have been evidenced in various rodent models of gastric and intestinal damage. VUF10460 is a non-imidazole agonist of histamine H4 receptor which binds to rat H4 receptor with a pKi of 7.46. VUF10460 displayed approximately a 50-fold selectivity for the rat H4 receptor over the H3 receptor. The ulcerogenic effect of immepip (a dual histamine H3/H4 receptor agonist) was mimicked by VUF10460 (10 mg/kg). Further, the aggravation of HCl-induced lesions observed after administration of VUF10460 was not significantly changed by JNJ7777120 (10 mg/kg; a histamine H4 receptor antagonist)[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.56mL

3.71mL

1.86mL

37.13mL

7.43mL

3.71mL
参考文献

[1]Coruzzi G, Adami M, et al. Selective histamine H₃ and H₄ receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur J Pharmacol. 2011 Nov 1;669(1-3):121-7.

[2]Cowart MD, Altenbach RJ, et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem. 2008 Oct 23;51(20):6547-57.

[3]Selective Histamine H3 and H4 Receptor Agonists Exert Opposite Effects Against the Gastric Lesions Induced by HCl in the Rat Stomach