Betahistine mesylate

Name: Betahistine mesylate
Brand: MedChemExpress
SKU: HY-D0237
Rating: 4.5 (1 reviews)

Cat. No.: HY-D0237 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).

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

Betahistine mesylate Chemical Structure

CAS No. : 54856-23-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Betahistine mesylate:

Betahistine dihydrochloride In-stock
Betahistine Get quote
Betahistine mesylate (Standard) Get quote

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist^[1]. Betahistine mesylate is used for the study of rheumatoid arthritis (RA)^[3].

IC₅₀ & Target

H₁ Receptor

H₃ receptor

In Vitro

Betahistine mesylate (0-10 μM) inhibits [¹²⁵I]iodoproxyfan binding to membranes of CHO (rH₃₍₄₄₅₎R) and CHO (hH₃₍₄₄₅₎R) cells with IC₅₀ values of 1.9 μM and 3.3 μM, respectively. Lead to K_i values of 1.4 μM and 2.5 μM, respectively^[2].
Betahistine mesylate (0-10 μM) has a regulating function on cAMP formation in CHO (rH₃₍₄₄₅₎R), CHO (rH₃₍₄₁₃₎R), and CHO (hH₃₍₄₄₅₎R) cells. At low concentrations, Betahistine mesylate behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC₅₀ values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, Betahistine mesylate inhibits cAMP formation with an EC₅₀ value of 0.1 μM in CHO (rH₃₍₄₄₅₎R) and full agonist activity^[2].

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

In Vivo

Betahistine mesylate (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED₅₀ of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED₅₀ of 2 mg/kg in male Swissmice^[2].
Betahistine mesylate (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice^[3].

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

Animal Model:	Collagen-induced arthritis (CIA) DBA/1 male mouse model^[3]
Dosage:	1 mg/kg; 5mg/kg
Administration:	Oral adminstration; day 21 to day 42 after a 21-day CIA induction
Result:	Ameliorated mouse CIA by decreasing joint destruction.

Clinical Trial

Molecular Weight

328.41

Formula

C₁₀H₂₀N₂O₆S₂

CAS No.

54856-23-4

Appearance

Solid

Color

White to off-white

SMILES

CNCCC1=NC=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (304.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0450 mL	15.2249 mL	30.4497 mL
5 mM	0.6090 mL	3.0450 mL	6.0899 mL
10 mM	0.3045 mL	1.5225 mL	3.0450 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (7.61 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 (7.61 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (255 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Poyurovsky M, et al. The effect of Betahistine mesylate, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. [Content Brief]

[2]. Gbahou F, et al. Effects of Betahistine mesylate at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54. [Content Brief]

[3]. Tang KT, et al. Betahistine mesylate attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0450 mL	15.2249 mL	30.4497 mL	76.1244 mL
	5 mM	0.6090 mL	3.0450 mL	6.0899 mL	15.2249 mL
	10 mM	0.3045 mL	1.5225 mL	3.0450 mL	7.6124 mL
	15 mM	0.2030 mL	1.0150 mL	2.0300 mL	5.0750 mL
	20 mM	0.1522 mL	0.7612 mL	1.5225 mL	3.8062 mL
	25 mM	0.1218 mL	0.6090 mL	1.2180 mL	3.0450 mL
	30 mM	0.1015 mL	0.5075 mL	1.0150 mL	2.5375 mL
	40 mM	0.0761 mL	0.3806 mL	0.7612 mL	1.9031 mL
	50 mM	0.0609 mL	0.3045 mL	0.6090 mL	1.5225 mL
	60 mM	0.0507 mL	0.2537 mL	0.5075 mL	1.2687 mL
	80 mM	0.0381 mL	0.1903 mL	0.3806 mL	0.9516 mL
	100 mM	0.0304 mL	0.1522 mL	0.3045 mL	0.7612 mL