您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > CI-949
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:
 
CI-949
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。
CI-949图片
CAS NO:104961-19-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CI-949 是一种过敏介质释放抑制剂,可抑制组胺 (histamine),白三烯 C4/D4(LTC4/LTD4) 和血栓素 B2(TXB2) 的释放,IC50分别为 11.4 μM,0.5 μM 和 0.1 μM。
生物活性

CI-949 is an allergic mediator release inhibitor, which inhibitshistamine,leukotriene C4/D4(LTC4/LTD4), andthromboxane B2(TXB2)release withIC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.

IC50& Target[1]

TXB2

0.1 μM (IC50)

LTC4

0.5 μM (IC50)

LTD4

0.5 μM (IC50)

Histamine

 

体外研究
(In Vitro)

CI-949 inhibits, in a dose-dependent manner, the release of histamine, leukotriene, and thromboxane from human basophilic leukocytes challenged with anti-IgE. The IC50for inhibition of histamine release is 11.4 μM. Virtually complete inhibition of histamine release occurs at 100 μM, with negligible inhibition of release<3 μm. both ltc4/LTD4and TXB2release are inhibited at lower concentrations (IC50, 0.5 and 0.1 μM, respectively). Complete inhibition of leukotriene and thromboxane synthesis/release is obtained with 10 and 1 μM of CI-949, respectively. CI-949 is an effective inhibitor of release of all three mediators in response to this stimulus. The IC50s for inhibition of histamine, leukotriene, and thromboxane are 6.3, 2, and 0.1 μM for FMLP challenge[1]. CI-949 effectively inhibits the release of histamine and the synthesis or release of immunoreactive sulfidopeptide leukotrienes C4-D4and thromboxane B2from antigen-challenged lung fragments of of actively sensitized guinea-pigs. The IC50s are 26.7±2.8 μM for histamine, 2.7±2.4 μM for leukotriene, and 3.0±1.8 μM for thromboxane[2].

体内研究
(In Vivo)

Actively sensitized guinea-pigs are given i .p. doses of 30, 50, or 100 mg/kg of CI-949 between 20-120 min before aerosol challenge with antigen. A dose of 50 mg/kg i.p. of CI-949 protects conscious, aerosol-allergen challenged guinea-pigs for at least 1 h and 100 mg/kg i.p. or per os protects for at least 2 h. The animals are protected from collapse for at least I h after 50 and 100 mg/kg, and 100 mg/kg afforded complete protection up to 2h. An oral dose of 100 mg/kg at 2 h, but not at 4 h before challenge also inhibits collapse. A dose of 100 mg/kg at 4 h and again at 2 h before challenge is more effective than a single dose at 2 h[2].

分子量

392.41

Formula

C20H20N6O3

CAS 号

104961-19-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.