104961-19-5
- CAS号:104961-19-5
- 英文名:1H-Indole-2-carboxamide, 5-methoxy-3-(1-methylethoxy)-1-phenyl-N-2H-tetrazol-5-yl-
- 中文名:104961-19-5
- CBNumber:CB03339549
- 分子式:C20H20N6O3
- 分子量:392.4112
- MOL File:104961-19-5.mol
- 密度 :1.38±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :3.32±0.10(Predicted)
104961-19-5性质、用途与生产工艺
- 生物活性 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。
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靶点
TXB 2
0.1 μM (IC 50 )
LTC 4
0.5 μM (IC 50 )
LTD 4
0.5 μM (IC 50 )
Histamine
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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 IC 50 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 LTC 4 /LTD 4 and TXB 2 release are inhibited at lower concentrations (IC 50 , 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 IC 50 s 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 C 4 -D 4 and thromboxane B 2 from antigen-challenged lung fragments of of actively sensitized guinea-pigs. The IC 50 s are 26.7±2.8 μM for histamine, 2.7±2.4 μM for leukotriene, and 3.0±1.8 μM for thromboxane.
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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.
- 公司名称:范德(北京)生物科技有限责任公司
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- 国家:中国
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- 公司名称:北京新研汇医药研发有限公司
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- 公司名称:天津普西唐生物医药科技有限公司
- 联系电话:010-60605840 15801484223;
- 电子邮件:psaitong@jm-bio.com
- 国家:中国
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- 公司名称:TargetMol中国(陶术生物)
- 联系电话: 4008200310
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