Wy 49051

Wy 49051CAS号: 113418-56-7分子式: C28H33N5O3分子量: 487.59描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
Wy 49051 is an orally active antagonist of H1 receptor(IC50 of 44 nM).
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:45 mg/mL (92.29 mM)
生物活性
靶点
H1 receptor:44 nM
In vitro(体外研究)
Wy 49051 showed a great inhibitory effect on H1. At a concentration of 100 nM, it produced 92% inhibition of histamine-induced guinea pig ileal contraction. Wy 49051 is the most effective compound, with 700 times the potency of astemizole and 470 times the potency of hydroquinone. Wy 49051 also has high affinity for α1 receptor with IC50 of 8 nM[1].
In vivo(体内研究)
Wy 49051 shows against histamine-induced lethality in the guinea pig(ED50 of 1.91 mg/kg by po, 0.70 mg/kg by ip, and 0.01 mg/kg by iv). The duration of action of 24 is also favorable since there is no decrease in oral efficacy up to 18 h posttreatment[1].