Bilastine , 2mMinDMSO , 202189-78-4

CAS NO.：202189-78-4

Empirical Formula: C28H37N3O3

Molecular Weight: 463.62

MDL number: MFCD09837814

PRODUCT Properties

• Melting point: 202 °C
• Boiling point: 639.1±55.0 °C(Predicted)
• Density: 1.16±0.1 g/cm3(Predicted)
• storage temp.: Sealed in dry,Room Temperature
• Water Solubility: Insoluble in water
• solubility: DMSO:49.3(Max Conc. mg/mL);106.34(Max Conc. mM)
• pka: 4.40±0.10(Predicted)
• form: powder to crystal
• color: White to Light yellow

Description and Uses

Bilastine, a potent and selective histamine H1 receptor antagonist, was approved in Europe in 2010 for the treatment of allergic rhinoconjunctivitis (AR) and urticaria (hives or skin rash). The original synthesis of bilastine involves alkylation of 2-piperidinyl-1H-benzimidazole with a phenethyltosylate, the para position of which is substituted with a dimethyloxazoline moiety serving as a masked carboxylic acid group. Alkylation of the benzimidazole nitrogen with 2-chloroethyl ethyl ether followed by unmasking of the oxazoline moiety with sulfuric acid provided bilastine.
In two major clinical trials, bilastine was effective at relieving allergic rhinitis as assessed by measuring the severity of nasal (obstruction, rhinorrhea, itching, sneezing) and nonnasal (ocular itching, tearing, ocular redness, itching of ears, and/or palate) symptoms.

Labelled Bilastine. It is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• HS Code: 2933.39.4100