MedChemExpress LLC (MCE)

MedChemExpress - Model Desloratadine - 100643-71-8

Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria[1][2][3][4][5][6].

Desloratadine

MCE China：Desloratadine

Brand：MedChemExpress (MCE)

Cat. No.HY-B0539

CAS：100643-71-8

Synonyms：Sch34117

Purity：99.83%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

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

Description：Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.

In Vitro：Desloratadine (300 nmol/L-100 µmol/L) inhibits the release or production of multiple inflammatory mediators in cells with high affinity receptors for IgE[1]. Desloratadine (1-10 μM, 15 min) has an inhibitory effect on IGE-induced IL-4 and IL-13 secretion that is nearly 6-7 times greater than its inhibitory effect on histamine and LTC4 release[2]. Desloratadine (0.1-10 μmol/L, 1 h) dose-dependently inhibits platelet-activating factor (PAF)-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion to human umbilical vein endothelial cells[5]. Desloratadine (1, 10 and 50 μM, 30 min) inhibits the activation of eosinophils and mast cells in polyp tissues of patients with chronic sinusitis[6].

In Vivo：Desloratadine inhibits histamine-induced paw edema in a mouse inflammatory model in a dose-dependent manner (ED50=0.15 mg/kg; p.o.) and dose-dependently reduces the number of coughs after ovalbumin (HY-W250978) sensitization and antigen challenge in sensitized guinea pigs (the minimum effective antitussive dose is 0.3 mg/kg)[5].

IC50 & Target：H1 Receptor Human Endogenous Metabolite

References：

[1]. Geha, R.S. and E.O. Meltzer, Desloratadine: A new, nonsedating, oral antihistamine. J Allergy Clin Immunol, 2001. 107(4): p. 751-62. [Content Brief]

[2]. Schroeder, J.T., et al., Inhibition of cytokine generation and mediator release by human basophils treated with desloratadine. Clin Exp Allergy, 2001. 31(9): p. 1369-77. [Content Brief]

[3]. McClellan K, et al. Desloratadine. Drugs. 2001;61(6):789-797. [Content Brief]

[4]. Anthes, J.C., et al., Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol, 2002. 449(3): p. 229-37. [Content Brief]

[5]. Agrawal, et al. "Pharmacology and clinical efficacy of desloratadine as an anti-allergic and anti-inflammatory drug." Expert opinion on investigational drugs 10.3 (2001): 547-560. [Content Brief]

[6]. Kowalski, et al. "Inhibition of nasal polyp mast cell and eosinophil activation by desloratadine." Allergy 60.1 (2005): 80-85. [Content Brief]

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