Wy 49051 是一种有效的，具有口服活性的 H1 receptor 拮抗剂，IC50 值为 44 nM。

Wy 49051 is an orally active antagonist of H1 receptor(IC50 of 44 nM).

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].

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].

113418-56-7

C28H33N5O3

487.59

Wy-49051

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years