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Desloratadine

🥰Excellent
Catalog No. T2520Cas No. 100643-71-8
Alias 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.

Desloratadine

Desloratadine

🥰Excellent
Purity: 100%
Catalog No. T2520Alias Sch34117, NSC 675447Cas No. 100643-71-8
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.
Pack SizePriceAvailabilityQuantity
25 mg$35In Stock
50 mg$46In Stock
100 mg$63In Stock
200 mg$101In Stock
500 mg$241In Stock
1 g$383In Stock
1 mL x 10 mM (in DMSO)$52In Stock
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Purity:100%
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Product Introduction

Bioactivity
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.
AliasSch34117, NSC 675447
Chemical Properties
Molecular Weight310.82
FormulaC19H19ClN2
Cas No.100643-71-8
SmilesClC1=CC2=C(C=C1)\C(=C1\CCNCC1)C1=C(CC2)C=CC=N1
Relative Density.1.221 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 31.1 mg/mL (100 mM)
DMSO: 40 mg/mL (128.69 mM), Sonication is recommended.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.2173 mL16.0865 mL32.1730 mL160.8648 mL
5 mM0.6435 mL3.2173 mL6.4346 mL32.1730 mL
10 mM0.3217 mL1.6086 mL3.2173 mL16.0865 mL
20 mM0.1609 mL0.8043 mL1.6086 mL8.0432 mL
50 mM0.0643 mL0.3217 mL0.6435 mL3.2173 mL
100 mM0.0322 mL0.1609 mL0.3217 mL1.6086 mL

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