108427-72-1
- CAS号:108427-72-1
- 英文名:AS 35
- 中文名:108427-72-1
- CBNumber:CB51385475
- 分子式:C21H20N6O4
- 分子量:420.42
- MOL File:108427-72-1.mol
- 熔点 :269-271 °C
- 沸点 :678.8±65.0 °C(Predicted)
- 密度 :1.46±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?+-.0.10(Predicted)
108427-72-1性质、用途与生产工艺
- 生物活性 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。
-
靶点
LTE 4
3 nM (IC 50 , In isolated guinea pig ileum)
LTD 4
4 nM (IC 50 , In isolated guinea pig ileum)
LTC 4
8 nM (IC 50 , In isolated guinea pig ileum)
-
体外研究
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.
-
体内研究
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.
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