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Merck
CN

SML2929

Bilastine

≥98% (HPLC)

Synonym(s):

2-[4-(2-(4-(1-(2-ethoxyethyl)benzimidazole-2-yl)piperidine-1-yl)ethyl)phenyl]-2-methyl-propanoic acid, 4-[2-[4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethylbenzeneacetic acid, F-96221-BM1

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About This Item

Empirical Formula (Hill Notation):
C28H37N3O3
CAS Number:
202189-78-4
Molecular Weight:
463.61
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD09837814

Key Documents

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Product Name

Bilastine, ≥98% (HPLC)

SMILES string

[N+H]2(CCC(CC2)c3[n](c4c(n3)cccc4)CCOCC)CCc1ccc(cc1)C(C)(C)C(=O)[O-]

InChI

1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33)

InChI key

ACCMWZWAEFYUGZ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Bilastine is an orally available, potent and selective histamine H1 receptor antagonist that exhibits long drug-target residence time at H1 receptor (73 min), which results in extended H1 receptor antagonism in vitro. Bilastine is used for treatment of allergic rhinitis and urticaria (hives).
orally available, potent and selective histamine H1 receptor antagonist that exhibits long drug-target residence time at H1 receptor

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000514310
0000514310
0000449409
0000449409
0000231291

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Reyes Corcóstegui et al.
Drugs in R&D, 6(6), 371-384 (2005-11-09)
This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist. In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using
Xue Yan Wang et al.
Therapeutics and clinical risk management, 12, 585-597 (2016-04-26)
Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged
Reggie Bosma et al.
European journal of pharmacology, 838, 107-111 (2018-09-12)
Drug-target binding kinetics has recently attracted considerable interest in view of the potential predictive power for in vivo drug efficacy. The recently introduced antihistamine bilastine has a long duration of in vivo drug action, which outlasts pharmacological active bilastine concentrations

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