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CI-949  

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包装规格：25mg 50mg 100mg in glass bottle
产品简介：一种选择性，有口服活性和脑渗透性的OX2R拮抗剂pKi值为7.85。
靶点：TXB2:0.1 μM (IC50);LTC4:0.5 μM (IC50);LTD4:0.5 μM (IC50);Histamine
体外研究：CI-949 inhibits, in a dose-dependent manner, the release of histamine, leukotriene, and thromboxane from human basophilic leukocytes challenged with anti-IgE. The IC50 for 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/LTD4 and TXB2 release 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. CI-949 effectively inhibits the release of histamine and the synthesis or release of immunoreactive sulfidopeptide leukotrienes C4-D4 and thromboxane B2 from 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.
体内研究：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.
保存条件：-20℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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