Betahistine dihydrochloride

Cat. No.: HY-B0524A Purity: 99.74%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Betahistine dihydrochloride Chemical Structure

CAS No. : 5579-84-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
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
1 g	USD 30	In-stock	Estimated Time of Arrival: December 31
5 g	USD 65	In-stock	Estimated Time of Arrival: December 31
10 g		Get quote
50 g		Get quote

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Other Forms of Betahistine dihydrochloride:

Betahistine In-stock
Betahistine-d₃ dihydrochloride In-stock
Betahistine mesylate In-stock
Betahistine-¹³C,d₃ dihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
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Description

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

IC₅₀ & Target^[1]

H₃ Receptor

In Vitro

Betahistine dihydrochloride (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 dihydrochloride (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 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 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 dihydrochloride (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 dihydrochloride (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

209.12

Formula

C₈H₁₄Cl₂N₂

CAS No.

5579-84-0

Appearance

Solid

Color

White to off-white

SMILES

CNCCC1=CC=CC=N1.Cl.Cl

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:

H₂O : ≥ 50 mg/mL (239.10 mM)

DMSO : 33.33 mg/mL (159.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 5 mg/mL (23.91 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.7819 mL	23.9097 mL	47.8194 mL
5 mM	0.9564 mL	4.7819 mL	9.5639 mL
10 mM	0.4782 mL	2.3910 mL	4.7819 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.

* 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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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

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 150 mg/mL (717.29 mM); Clear solution; Need ultrasonic

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.

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

Purity: 99.74%

Select Batch:

Data Sheet (295 KB) SDS (393 KB)

COA (248 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Poyurovsky M, et al. The effect of betahistine, 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 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 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

DMF / DMSO / H₂O	1 mM	4.7819 mL	23.9097 mL	47.8194 mL	119.5486 mL
	5 mM	0.9564 mL	4.7819 mL	9.5639 mL	23.9097 mL
	10 mM	0.4782 mL	2.3910 mL	4.7819 mL	11.9549 mL
	15 mM	0.3188 mL	1.5940 mL	3.1880 mL	7.9699 mL
	20 mM	0.2391 mL	1.1955 mL	2.3910 mL	5.9774 mL
DMSO / H₂O	25 mM	0.1913 mL	0.9564 mL	1.9128 mL	4.7819 mL
	30 mM	0.1594 mL	0.7970 mL	1.5940 mL	3.9850 mL
	40 mM	0.1195 mL	0.5977 mL	1.1955 mL	2.9887 mL
	50 mM	0.0956 mL	0.4782 mL	0.9564 mL	2.3910 mL
	60 mM	0.0797 mL	0.3985 mL	0.7970 mL	1.9925 mL
	80 mM	0.0598 mL	0.2989 mL	0.5977 mL	1.4944 mL
	100 mM	0.0478 mL	0.2391 mL	0.4782 mL	1.1955 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.