| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| 10g |
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Purity: ≥98%
Betahistine mesylate (also known as PT-9), the mono-HCl salt of Betahistine, is a potent histamine H3 receptor inhibitor with IC50 of 1.9 μM. Betahistine dihydrochloride is a medication for vertigo. It is frequently prescribed to treat balance issues or to lessen Ménière's disease-related vertigo symptoms. In 1970, it received approval for the first time in Europe to treat Ménière's disease.
| ln Vitro |
Betahistine mesylate (0-10 μM) inhibits [125I]iodoproxyfan binding to the 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 Ki values of 1.4 μM and 2.5 μM, respectively[2].
Betahistine mesylate (0-10 μM) regulates the formation of cAMP in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. Betahistine mesylate exhibits apparent inverse agonistic behavior at low concentrations, gradually increasing the formation of cAMP with EC50 values of 0.1 nM, 0.05 nM, and 0.3 nM, respectively. On the other hand, betahistine mesylate, at concentrations greater than 10 nM, inhibits full agonist activity and the formation of cAMP in CHO (rH3(445)R) with an EC50 value of 0.1 μM[2]. |
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| ln Vivo |
Betahistine mesylate (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg after acute administration, suggesting the opposite agonism. Furthermore, in male Swissmice, it raises t-MeHA levels with an ED50 of 2 mg/kg following acute oral administration[2].
Betahistine mesylate (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) decreases the amount of pro-inflammatory cytoKines and lessens the severity of arthritis in the paw tissues of CIA mice[3]. |
| Animal Protocol |
Collagen-induced arthritis (CIA) DBA/1 male mouse model
1 mg/kg; 5mg/kg Oral adminstration; day 21 to day 42 after a 21-day CIA induction |
| References |
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| Molecular Formula |
C₁₀H₂₀N₂O₆S₂
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|---|---|
| Molecular Weight |
328.41
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| Exact Mass |
328.08
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| Elemental Analysis |
C, 36.57; H, 6.14; N, 8.53; O, 29.23; S, 19.53
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| CAS # |
54856-23-4
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| Related CAS # |
Betahistine; 5638-76-6; Betahistine dihydrochloride; 5579-84-0
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| Appearance |
Solid powder
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| SMILES |
CNCCC1=CC=CC=N1.CS(=O)(=O)O.CS(=O)(=O)O
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| InChi Key |
ZBJJDYGJCNTNTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H12N2.2CH4O3S/c1-9-7-5-8-4-2-3-6-10-8;2*1-5(2,3)4/h2-4,6,9H,5,7H2,1H3;2*1H3,(H,2,3,4)
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| Chemical Name |
methanesulfonic acid;N-methyl-2-pyridin-2-ylethanamine
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| Synonyms |
PT9; PT-9; BRN0112294; BRN-0112294; BRN 0112294; beta-Histine; Betahistine; NSC 42617; PT 9 base; Serc base
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1) .This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 65~100 mg/mL (197.9~304.5 mM))
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00160238 | Completed | Drug: Betahistine 24 mg bid (Betaserc) |
Meniere's Disease | Solvay Pharmaceuticals | January 2003 | Phase 4 |
| NCT00459992 | Completed | Drug: Betahistine Hydrochloride | Obesity Overweight |
Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) |
April 10, 2007 | Phase 1 |
| NCT05938517 | Completed | Drug: Betahistine dihydrochloride Drug: Selegiline-hydrochloride |
Ménière's Disease | Ludwig-Maximilians - University of Munich |
June 2, 2021 | Phase 1 |
| NCT01468285 | Completed | Drug: betahistine dihydrochloride Other: placebo |
Gait or Balance Disorder Problems | Abbott Products | February 2012 | Phase 4 |
| NCT00829881 | Completed | Drug: Betahistine Hydrochloride Drug: Placebo Capsule |
Attention Deficit Disorder With Hyperactivity |
P2D, Inc. | January 2009 | Phase 1 |
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