104961-19-5
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- CAS号:
- 104961-19-5
- 英文名:
- 1H-Indole-2-carboxamide, 5-methoxy-3-(1-methylethoxy)-1-phenyl-N-2H-tetrazol-5-yl-
- 英文别名:
- CI 949,CI949;1H-Indole-2-carboxamide, 5-methoxy-3-(1-methylethoxy)-1-phenyl-N-2H-tetrazol-5-yl-
- 中文名:
- 104961-19-5
- 中文别名:
- 化合物 T10054
- CBNumber:
- CB03339549
- 分子式:
- C20H20N6O3
- 分子量:
- 392.4112
- MOL File:
- 104961-19-5.mol
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104961-19-5化学性质
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密度:
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1.38±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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3.32±0.10(Predicted)
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104961-19-5性质、用途与生产工艺
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。
TXB
2
0.1 μM (IC
50
)
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LTC
4
0.5 μM (IC
50
)
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LTD
4
0.5 μM (IC
50
)
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Histamine
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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.
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.
104961-19-5
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上游原料
下游产品
104961-19-5, 104961-19-5 相关搜索:
- 化合物 T10054
- 104961-19-5
- CI 949,CI949
- 1H-Indole-2-carboxamide, 5-methoxy-3-(1-methylethoxy)-1-phenyl-N-2H-tetrazol-5-yl-