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Desloratadine

Catalog No. T2520 CAS 100643-71-8

Synonyms: Sch34117, NSC 675447

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

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Desloratadine, CAS 100643-71-8

Pack Size	Availability	Price/USD
25 mg	In stock	$ 35.00
50 mg	In stock	$ 46.00
100 mg	In stock	$ 63.00
200 mg	In stock	$ 101.00
500 mg	In stock	$ 241.00
1 g	In stock	$ 383.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 100%

Biological Description

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Description	Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.
Targets&IC50	H1 receptor:51 nM
In vitro	Desloratadine inhibits histamine-induced paw edema in mice, with an ED50 of 0.15 mg/kg, and exhibits dose-dependent and sustained mydriasis in guinea pigs in vivo at concentrations of 1 mg/mL, 3 mg/mL, and 10 mg/mL. It also suppresses the increase in vascular permeability in guinea pigs caused by histamine assault on the upper respiratory tract, with an ED50 of 0.9 μg. Furthermore, 5 mg/kg desloratadine counteracts the disruption of the blood-brain barrier in awake mice, thereby inhibiting tremors induced by the tremogenic agent oxotremorine.
In vivo	Desloratadine acts as a competitive antagonist to carbachol-induced contractions in isolated rabbit iris sphincter muscles, with a pA2 of 6.67. It binds to the human H1 receptor with a Ki value of 0.87 nM, displacing tritiated mepyramine. In competitive binding studies, Desloratadine was found to be more effective than cetirizine, ebastine, fexofenadine, and loratadine by factors of 52, 57, 194, and 153, respectively. Desloratadine (0.1 μM to 10 μM) also inhibits platelet-activating factor-induced chemotaxis and TNF-α-induced adhesion of eosinophils in patients with allergic rhinitis or asthma. Furthermore, it dose-dependently reduces IL-13 secretion from human basophils activated by IL-3 and PMA across the same concentration range. Pre-treatment with Desloratadine at 10 μM results in an approximately 80% reduction in anti-IgE-induced accumulation of IL-4 messages in cultured basophils. [3H]Desloratadine binds to human histamine H1 receptors expressed in CHO cells with a Kd of 1.1 nM. Concentrations of Desloratadine ranging from 100 nM to 10 μM were found to inhibit both IgE-mediated and non-IgE-mediated production of cytokines IL-4 and IL-13 in human basophils. Additionally, Desloratadine at 300 nM to 100 μM inhibits the release of histamine from human peripheral blood basophils stimulated by both IgE-mediated and non-IgE-mediated pathways.

Synonyms	Sch34117, NSC 675447
Molecular Weight	310.82
Formula	C19H19ClN2
CAS No.	100643-71-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 31.1 mg/mL (100 mM)

DMSO: 6.2 mg/mL (20 mM)

References and Literature

1. 1. Cardelús I, et al. Eur J Pharmacol. 1999 Jun 18;374(2):249-54. 2. Geha RS, et al. J Allergy Clin Immunol, 2001, 107(4), 751-762. 3. Schroeder JT, et al. Clin Exp Allergy, 2001, 31(9), 1369-1377. 4. Anthes JC, et al. Eur J Pharmacol, 2002, 449(3), 229-237. 5. Howell G 3rd, et al. BMC Pharmacol, 2005, 5, 13. 6. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

Citations

1. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 2. Wang D, Guo Q, Wu Z, et al.Molecular mechanism of antihistamines recognition and regulation of the histamine H1 receptor.Nature Communications.2024, 15(1): 84.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library EMA Approved Drug Library Membrane Protein-targeted Compound Library Anti-Cancer Clinical Compound Library GPCR Compound Library Anti-Cancer Approved Drug Library NO PAINS Compound Library Histamine & Melatonin Receptor-Targeted Compound Library

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Keywords

Desloratadine 100643-71-8 GPCR/G Protein Immunology/Inflammation Metabolism Neuroscience Endogenous Metabolite Histamine Receptor NSC675447 Sch 34117 inhibit Sch34117 Sch-34117 NSC 675447 Inhibitor NSC-675447 inhibitor

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