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, can suppress the expression of nerve growth factor (NGF). 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

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 55 In-stock
Estimated Time of Arrival: December 31
Solid
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
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Bepotastine besilate:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bepotastine besilate

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3][4].

IC50 & Target

Histamine H1 receptor[1][2][3][4].

In Vitro

Bepotastine besilate (10, 100, 1000 µM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 µM[1].
Bepotastine besilate (50 µM; 1 h) suppresses the expression of NGF mRNA in NHEKs[2].

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

Cell Viability Assay[2]

Cell Line: NHEKs
Concentration: 50 µM (preincubation)
Incubation Time: 1 h
Result: Suppressed the expression of NGF mRNA in NHEKs.

Western Blot Analysis[1]

Cell Line: RPMCs
Concentration: 10, 100, 1000 µM
Incubation Time: 120 min (preincubate)
Result: Decreased the release of histamine.
In Vivo

Bepotastine besilate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration[1].
Bepotastine besilate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control[3].
Bepotastine besilate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash[3].

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

Animal Model: Guinea pigs (6-week-old)[1].
Dosage: 10 g/L (1.0% (w/v)) for 10 µL.
Administration: Eye drop; 3 times at intervals of 20 min (in one eye).
Result: Inhibited PAF-induced conjunctival eosinophil infiltration.
Animal Model: Male BALB/c mice(12-week-old); NC/Nga mice[3].
Dosage: 3, 10 mg/kg
Administration: Oral administration; once (1 h before induces scratching behavior of Male BALB/c mice).
Result: Significantly inhibited histamine-mediated scratching behavior in male BALB/c mice.
Significantly suppressed serum LTB 4 levels in NC/Nga mice with a rash.
Clinical Trial
Molecular Weight

547.06

Formula

C27H31ClN2O6S

CAS No.
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 available by MCE.
Purity & Documentation

Purity: 99.65%

References
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Bepotastine besilate
Cat. No.:
HY-A0015
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