产品描述
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum. With IC50 values of 8 nM, 4 nM and 3 nM, respectively. It has antiallergic activities.
体外活性
In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC50 values of 10 nM and 20 nM, respectively. In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively. AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate[1].
体内活性
AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig[1]. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. 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.
Cas No.
108427-72-1
分子式
C21H20N6O4
分子量
420.42
别名
AS-35
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years