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Wy 49051
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Wy 49051图片
CAS NO:113418-56-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
Wy49051是一种有效的,可口服的H1receptor拮抗剂,IC50值为44nM。
Cas No.113418-56-7
Canonical SMILESO=C(N1C)N(C)C2=C(N(CCCN3CCC(OC(C4=CC=CC=C4)C5=CC=CC=C5)CC3)C=N2)C1=O
分子式C28H33N5O3
分子量487.59
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.

Wy 49051 shows great inhibitory effect on H1, producing 92% inhibition of the histamine-induced contraction of the guinea pig ileum at a concentration 100 nM. Wy 49051 is the most potent compound with 700 times the potency of astemazole, 470 times the potency of chlorpheniramine. Wy 49051 also has high affinity for α1 receptor with IC50 of 8 nM[1].

Wy 49051 shows potent activity against histamine-induced lethality in the guinea pig, with 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].

[1]. Abou-Gharbia M, et al. New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists. J Med Chem. 1995 Sep 29;38(20):4026-32.