Wy 49051 

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

IC50: 44 nM (H1 receptor)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

487.59

C₂₈H₃₃N₅O₃

113418-56-7

O=C(N1C)N(C)C2=C(N(CCCN3CCC(OC(C4=CC=CC=C4)C5=CC=CC=C5)CC3)C=N2)C1=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]