Bepotastine Besilate

Synonyms: TAU 284

Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

Bepotastine Besilate Chemical Structure

Bepotastine Besilate Chemical Structure

CAS: 190786-44-8

Selleck's Bepotastine Besilate has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.86%
99.86

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Biological Activity

Description Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
Targets
Histamine H1 receptor [1]
5.7(pIC50)
In vitro
In vitro The flux ratios of [14C]Bepotastine (5 μM) in LLC-GA5-COL150 cells are significantly greater than those in LLC-PK1, showing that the B-to-A flux exceeds those in the other direction in LLC-GA5-COL150 cells. Bepotastine stimulates P-gp-mediated ATP hydrolysis with Km, Vmax, and Vmax/Km values of 1.25 mM, 108 nmol/min/mg protein, and 0.087 mL/min/mg protein, respectively. [2] Bepotastine besilate (100 mM) suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured dorsal root ganglion neurons and cultured neutrophils. [3] Bepotastine (100 μM) dose-dependently inhibits chemotaxis of cultured guinea pig peritoneal eosinophils induced by LTB4. Bepotastine (1 mM) significantly reduces A23187-induced histamine release of cultured rat peritoneal mast cells. [4]
In Vivo
In vivo Bepotastine (0.8 mg/kg) administrated in WT and P-gp KO mice results in the plasma total concentrations 580 ng/mL and 467 ng/mL at 6 min after dosing, respectively, and the plasma protein binding with 41.1% and 45.9%. The absorption of [14C]Bepotastine from the proximal region in the presence and absence of verapamil is 63.0% and 72.4%, respectively, and that from the distal region is 10.9% and 62.7%, respectively. [2] Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site). Bepotastine besilate (1 mg/kg-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B(4) (0.03 nmol/site). [3] Bepotastine besilate significantly inhibits conjunctival vascular hyperpermeability in a dose-dependent manner in guinea pig allergic conjunctivitis models with maximal effect for Bepotastine besilate 1.5%. [4] Bepotastine (3 mg/kg and 10 mg/kg) effectively inhibits the compound 48/80-induced scratching behavior of BALB/c mice 1 hour after oral administration. Bepotastine (10 mg/kg) also significantly inhibits the scratching behavior and suppresses the serum LTB(4) levels in atopic dermatitis model NC/Nga mice. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01925313 Completed
Healthy
HK inno.N Corporation
December 2012 Phase 1
NCT01425632 Completed
Perennial Allergic Rhinitis
Mitsubishi Tanabe Pharma Corporation
August 2011 Phase 3

Chemical Information & Solubility

Molecular Weight 547.06 Formula

C21H25ClN2O3.C6H6O3S

CAS No. 190786-44-8 SDF Download Bepotastine Besilate SDF
Smiles C1CN(CCC1OC(C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O.C1=CC=C(C=C1)S(=O)(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 109 mg/mL ( (199.24 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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