您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
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。
CAS NO:1082954-71-9
包装与价格:
包装价格(元)
5 mg电议
50 mg电议
100 mg电议

产品介绍
A-987306 是一种高效、口服生物可利用的组胺H4拮抗剂,对大鼠和人 H4作用的Ki值分别为 3.4 nM 和 5.8 nM。 A-987306 在小鼠腹膜炎模型中显示出抗炎活性。

产品描述

A-987306 is a potent and oral bioavailable histamine H 4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 exhibits anti-inflammatory activity in mice peritonitis model [1].

体外活性

A-987306 is a potent and functional antagonist in vitro of human, rat, and mouse H4 receptors in cell-based FLIPR assays [1]. A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H 4 R over the human H 1, H 2, and H 3 receptors in cell-based Ca 2+ -flux functional assay (FLIPR) [1]. A-987306 shows lower selectivity for H 4 R in the rat (only 4-fold selective for the rat H 4 R over the rat H 3 R) in FLIPR [1].

体内活性

A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) has been shown to reduce scratching induced by the histamine H 4 agonist clobenpropit [1]. A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (F po/iv =26%) with a half-life of 3.7 h and a C max of 0.30 μM at a T max of 1.5 h after dosing [1]. Animal Model: Mice [1] Dosage: 98.23 μg/kg, 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis) Administration: Intraperitoneal injection Result: F po/iv =26%, T 1/2 =3.7 hours, C max =0.30 μM, T max =1.5 hours

Cas No.

1082954-71-9

分子式

C18H25N5O

分子量

327.42

别名

A 987306

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years