Bepotastine Besilate

Catalog No.S3037 Synonyms: TAU 284

Bepotastine Besilate Chemical Structure

Molecular Weight(MW): 547.06

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

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In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
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Biological Activity

Description Bepotastine 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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 109 mg/mL (199.24 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 547.06
Formula

C21H25ClN2O3.C6H6O3S

CAS No. 190786-44-8
Storage powder
Synonyms TAU 284

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01900054 Completed Perennial Allergic Rhinitis Mitsubishi Tanabe Pharma Corporation June 2013 Phase 3
NCT01861522 Completed Perennial Allergic Rhinitis Mitsubishi Tanabe Pharma Corporation April 2013 Phase 3
NCT01840605 Completed Dermatitis|Atopic Mitsubishi Tanabe Pharma Corporation March 2013 Phase 3
NCT01753739 Completed Seasonal Allergic Rhinitis Bausch & Lomb Incorporated January 2013 Phase 2
NCT01578278 Completed Seasonal Allergic Rhinitis Bausch & Lomb Incorporated December 2011 Phase 2
NCT01443442 Completed Allergic Conjunctivitis Southern California College of Optometry October 2011 Phase 4

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID