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

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

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

Bepotastine Chemical Structure

Bepotastine Chemical Structure

CAS No. : 125602-71-3

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Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 68 In-stock
Solution
10 mM * 1 mL in DMSO USD 68 In-stock
Liquid
5 mg USD 62 In-stock
10 mg USD 93 In-stock
25 mg USD 186 In-stock
50 mg USD 280 In-stock
100 mg USD 420 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Bepotastine:

Bepotastine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bepotastine

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

Histamine H1 Receptor[1][2][3]
In Vitro

Bepotastine (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 (50 µM; 1 h) suppresses the expression of NGF mRNA in NHEKs[2].

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

Bepotastine Related Antibodies

Cell Viability Assay[1]

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

Western Blot Analysis[2]

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

Bepotastine (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 (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 (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].

MedChemExpress (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

388.89

Formula

C21H25ClN2O3
CAS No.
Appearance

Liquid (Density: 1.26 g/cm3)

Color

Light brown to brown

SMILES

O=C(O)CCCN1CCC(O[C@@H](C2=CC=C(Cl)C=C2)C3=CC=CC=N3)CC1
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: 

H2O : ≥ 100 mg/mL (257.14 mM)

DMSO : 100 mg/mL (257.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5714 mL 12.8571 mL 25.7142 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.5714 mL 12.8571 mL 25.7142 mL 64.2855 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL 12.8571 mL
10 mM 0.2571 mL 1.2857 mL 2.5714 mL 6.4286 mL
15 mM 0.1714 mL 0.8571 mL 1.7143 mL 4.2857 mL
20 mM 0.1286 mL 0.6429 mL 1.2857 mL 3.2143 mL
25 mM 0.1029 mL 0.5143 mL 1.0286 mL 2.5714 mL
30 mM 0.0857 mL 0.4286 mL 0.8571 mL 2.1429 mL
40 mM 0.0643 mL 0.3214 mL 0.6429 mL 1.6071 mL
50 mM 0.0514 mL 0.2571 mL 0.5143 mL 1.2857 mL
60 mM 0.0429 mL 0.2143 mL 0.4286 mL 1.0714 mL
80 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8036 mL
100 mM 0.0257 mL 0.1286 mL 0.2571 mL 0.6429 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Bepotastine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bepotastine125602-71-3Histamine Receptorpruritusatopic dermatitisurticariaLTB 4conjunctivitisADInhibitorinhibitorinhibit

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