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MedChemExpress - Model Emedastine difumarate -87233-62-3

Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].

Emedastine difumarate

MCE China：Emedastine difumarate

Brand：MedChemExpress (MCE)

Cat. No.HY-B2178

CAS：87233-62-3

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

In Vitro：Emedastine difumarate inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM)[1]. High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2]. Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].

In Vivo：Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg[3]. Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3]. Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2]. Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].

IC50 & Target：H1 Receptor 1.3 nM (Ki) H2 Receptor 49067 nM (Ki) H3 Receptor 12430 nM (Ki)

References：

[1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64. [Content Brief]

[2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. [Content Brief]

[3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52. [Content Brief]

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MedChemExpress - Model Emedastine difumarate -87233-62-3

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Emedastine difumarate