货号 | 2441/50 |
别名 | 1-[(5-Chloro-1H-benzimidazol-2-yl)c |
供应商 | Tocris |
生物活性 | Highly selective histamine H4 receptor silent antagonist; binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). Inhibits mast cell and eosinophil chemotaxis in vitro with IC50 values of 138 and 530 nM respectively. Orally active in vivo. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >99 % |
计算分子量 | 394.81 |
分子式 | C13H15ClN4O.C4H4O4 |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
CAS号 | 869497-75-6 |
参考文献 | Vargaet al (2005) Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur.J.Pharmacol. 522 130. PMID: 16213481. Venableet al (2005) Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists. J.Med.Chem. 48 8289. PMID: 16366610. Terziogluet al (2004) Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists. Bioorg.Med.Chem.Lett. 14 5251. PMID: 15454206. |