您好，欢迎来到试剂仪器网！ [登录] [免费注册]
试剂仪器网
发布求购
位置：首页 > 产品库 > A 987306
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
A 987306
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A 987306图片
CAS NO:1082954-71-9
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
A 987306 是一种有效的、可口服的组胺 H4 拮抗剂，对大鼠 H4 和人 H4 的 Kis 分别为 3.4 nM 和 5.8 nM。
Cas No.1082954-71-9
化学名(7aR,11aR)-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine
Canonical SMILESNC(N=C1N2CCNCC2)=NC3=C1CCC4=C3[C@@H](CCCC5)[C@@H]5O4
分子式C18H25N5O
分子量327.42
溶解度<32.74mg/ml in DMSO;<32.74mg/ml in ethanol
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A987306,cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quin- azolin-2-amine[1], is a selective and potent H4 receptor antagonist [2].

H4R is one of 4 known G-protein-coupled receptors (H1, H2, H3 and H4 receptors) of histamine. It is for mediating some physiological functions of histamine [3].

In a cell-based Ca2+-flux functional assay, A 987306 had no activation to the receptor, but blocked the H4R activation induced by endogenous histamine. A 987306 potently decreased histamine-mediated binding between rat H4-receptor-containing membranes and GTP-γ-[35S] with a Kb of 6 nM [3].

In Sprague-Dawley rats, after ip injection, A 987306 had a favorable fractional bioavailability (Fip/iv =72%), a half-life of 4.7 h and a Cmax of 1.73 μM at a Tmax of 0.25 h after dosing. After oral dosing, A 987306 had a moderate fractional oral bioavailability (Fpo/iv =26%) with a half-life of 3.7 h and a Cmax of 0.30 μM at a Tmax of 1.5 h after dosing. The plasma protein binding of A 987306 measured in rats was found to be 59% [3].

To human H4R and rat H4R, the Ki values of A 987306 are 5.8 nM and 3.4 nM, respectively. A 987306 reduced scratch responses in mice with an ED50 of 0.36 μmol/kg. A 987306 was found to be selective and bear an IC50 >810 nM for over 100 kinases [3].

References:
[1].  Vanina A. Medina and Elena S. Rivera. Histamine receptors and cancer pharmacology. British Journal of Pharmacology, 2010, 161:755-767.
[2].  M.I. Strakhova, C.A. Cuff, A.M. Manelli, et al. In vitro and in vivo characterization of A-940894: a potent histamine H4 receptor antagonist with anti-inflammatory properties. British Journal of Pharmacology, 2009, 157:44-54.
[3].  Huaqing Liu, Robert J. Altenbach, Tracy L. Carr, et al. cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia. J. Med. Chem., 2008, 51:7094-7098.