1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Bepotastine besilate

Bepotastine besilate 

Cat. No.: HY-A0015 Purity: 99.65%
Handling Instructions

Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.

For research use only. We do not sell to patients.

Bepotastine besilate Chemical Structure

Bepotastine besilate Chemical Structure

CAS No. : 190786-44-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
Estimated Time of Arrival: December 31
50 mg USD 190 In-stock
Estimated Time of Arrival: December 31
100 mg USD 300 In-stock
Estimated Time of Arrival: December 31
500 mg USD 850 In-stock
Estimated Time of Arrival: December 31
1 g   Get quote  
5 g   Get quote  

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Description

Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2].

IC50 & Target

Histamine H1 receptor[1]

In Vitro

Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function, inhibition of eosinophilic infiltration, inhibition of IL-5 production, and inhibition of leukotriene B4 (LTB4) and LTD4 activity[1].
Bepotastine significantly inhibits antigen-induced stimulation of IL-5 production in human peripheral blood mononuclear cells (PBMCs) at concentrations of 10-100 μM and the effect is enhanced when the PBMCs are pre-incubated with Bepotastine[1].
Leukotriene B4 increased Ca2+ concentration in cultured neutrophils, which is suppressed by Bepotastine besilate (1-100 μM). Leukotriene B4 increased Ca2+ concentration in cultured dorsal root ganglion neurons, which is also suppressed by Bepotastine besilate (100 μM)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site)[2].
Bepotastine besilate (1-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B4 (0.03 nmol/site)[2]. Bepotastine in vivo dose-dependently inhibits the acceleration of histamine-induced vascular permeability and inhibits homologous passive cutaneous anaphylaxis in guinea pig studies[1].
In mouse models of itching, oral Bepotastine inhibits the frequency and duration of scratching behavior[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

547.06

Formula

C₂₇H₃₁ClN₂O₆S

CAS No.

190786-44-8

SMILES

O=C(CCCN1CCC(CC1)O[[email protected]](C2=NC=CC=C2)C3=CC=C(C=C3)Cl)O.O=S(C4=CC=CC=C4)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (182.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8280 mL 9.1398 mL 18.2795 mL
5 mM 0.3656 mL 1.8280 mL 3.6559 mL
10 mM 0.1828 mL 0.9140 mL 1.8280 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.65%

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Keywords:

BepotastineHistamine ReceptorP-glycoproteinTRPV1non-sedatingallergicrhinitisconjunctivitisurticariapruritushistamine-H1leukotrieneB4Inhibitorinhibitorinhibit

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Bepotastine besilate
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