Bepotastine Besilate

SKU: orb1300797

Description

Bepotastine Besilate (TAU 284) is a selective, non-sedating histamine H1 receptor antagonist (pIC50: 5.7). It is used in research to study allergic responses and inflammation, with applications in both in vitro binding assays and in vivo models of allergic conjunctivitis and dermatitis.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 190786-44-8
• MW: 547.06
• Purity: 99.90%
• Formula: C₂₁H₂₅ClN₂O₃·C₆H₆O₃S
• SMILES: OS(=O)(=O)c1ccccc1.OC(=O)CCCN1CCC(CC1)O[C@@H](c1ccc(Cl)cc1)c1ccccn1
• Target: Histamine Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.31 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:101 mg/mL (184.62 mM)

Bioactivity

• Target IC50:
  H1 receptor:5.7(pIC50)
• 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. 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). 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%. 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.
• 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. Bepotastine besilate (100 mM) suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured dorsal root ganglion neurons and cultured neutrophils. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LTB 4, Inhibitor, inhibit, H1 receptor, HistamineReceptor, Histamine Receptor, atopic dermatitis, conjunctivitis, Bepotastine, Bepotastine Besilate, Bepotastine Beslilate, Bepreve, pruritus, Talion, TAU284, TAU-284, TAU 284, urticaria

Compound Identifiers

PubChem CID

164521