Bilastine

Catalog No.S3721 Batch:S372101

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Technical Data

Formula

C28H37N3O3

Molecular Weight 463.61 CAS No. 202189-78-4
Solubility (25°C)* In vitro 4-Methylpyridine 29 mg/mL (62.55 mM)
DMSO 1 mg/mL (2.15 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
Targets
H1 receptor [2]
(in guinea-pig cerebellum)
44.15 nM(Ki)
In vitro Bilastine has a high specific affinity for the H1-receptor but it has no or very low affinity for 30 other tested receptors[1]. It is lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3- receptors[2].
In vivo Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms in patients with allergic rhinoconjunctivitis. Bilastine is well tolerated. In the fasting state bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice. In vivo studies in rats have demonstrated reduction in histamine-stimulated smooth muscular contraction, bronchospasms, endothelial permeability, and microvascular extravasation[1].

Protocol (from reference)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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