108427-72-1
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- CAS号:
- 108427-72-1
- 英文名:
- AS 35
- 英文别名:
- AS 35;AS 35,AS35;4H-Pyrido[1,2-a]pyrimidin-4-one, 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)-;3-(1H-Tetrazol-5-yl)-9-[[[2-propyl-3-hydroxy-4-(methylcarbonyl)phenyl]oxy]methyl]-4H-pyrido[1,2-a]pyrimidin-4-one
- 中文名:
- 108427-72-1
- 中文别名:
- 化合物 T14326
- CBNumber:
- CB51385475
- 分子式:
- C21H20N6O4
- 分子量:
- 420.42
- MOL File:
- 108427-72-1.mol
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108427-72-1化学性质
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熔点:
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269-271 °C
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沸点:
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678.8±65.0 °C(Predicted)
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密度:
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1.46±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?+-.0.10(Predicted)
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108427-72-1性质、用途与生产工艺
AS-35 是一种有效的，可口服的，选择性的 leukotrienes 拮抗剂，抑制 LTC4，LTD4 和 LTE4 诱导的回肠收缩, IC50 值分别为 8 nM，4 nM 和 3 nM，具有抗过敏的功效。
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LTE
4
3 nM (IC
50
, In isolated guinea pig ileum)
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LTD
4
4 nM (IC
50
, In isolated guinea pig ileum)
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LTC
4
8 nM (IC
50
, In isolated guinea pig ileum)
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In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC
50
values of 8 nM, 4 nM and 3 nM, respectively. In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC
50
values of 10 nM and 20 nM, respectively. However, AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate.
AS-35 (0.0375 to 0.3 mg/kg, i.v.) dose-dependently antagonizes bronchoconstriction induced by i.v.-injection of LTC4 and LTD4 in anesthetized guinea pigs, but does not inhibit histamine-induced bronchoconstriction. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig.
108427-72-1
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108427-72-1, 108427-72-1 相关搜索:
- 化合物 T14326
- 108427-72-1
- AS 35,AS35
- 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)-
- 3-(1H-Tetrazol-5-yl)-9-[[[2-propyl-3-hydroxy-4-(methylcarbonyl)phenyl]oxy]methyl]-4H-pyrido[1,2-a]pyrimidin-4-one
- AS 35