Bepotastine Besilate
Catalog No.S3037 Synonyms: TAU 284
Molecular Weight(MW): 547.06
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
Purity & Quality Control
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Biological Activity
| Description | Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. | ||
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| Targets |
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| 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] |
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| 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 |
| in solvent | |
| Synonyms | TAU 284 |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02332044 | Completed | Healthy | Daewoong Pharmaceutical Co. LTD. | April 2014 | Phase 1 |
| NCT01753739 | Completed | Seasonal Allergic Rhinitis | Bausch & Lomb Incorporated | January 2013 | Phase 2 |
| NCT01925313 | Completed | Healthy | CJ HealthCare Corporation | December 2012 | Phase 1 |
| NCT01578278 | Completed | Seasonal Allergic Rhinitis | Bausch & Lomb Incorporated | December 2011 | Phase 2 |
| NCT01337557 | Unknown status | Allergic Conjunctivitis | Hom Milton M. OD FAAO|Bausch & Lomb Incorporated | May 2011 | Phase 4 |
| NCT01897428 | Completed | Allergic Rhinitis|Urticaria|Pruritus | Korea University Anam Hospital|Hanlim Pharm. Co. Ltd. | April 2011 | Phase 1 |
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