| 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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| 2g |
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| 5g |
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| Other Sizes |
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Purity: ≥98%
| ln Vitro |
With IC50 values of 1.9 μM and 3.3 μM, respectively, betahistine (0-10 μM) inhibits the binding of [125I]iodoproxyfan to CHO (rH3(445)R) and CHO (hH3(445)R) cell membranes. The corresponding Ki values are 2.5 μM and 1.4 μM [2]. The generation of cAMP in CHO (rH3(445)R), CHO (rH3(413)R, and CHO (hH3(445)R) cells is modulated by betahistine (0-10 μM). Betahistine exhibits clear inverse agonistic properties at low doses, progressively increasing the production of cAMP at EC50 values of 0.1 nM, 0.05 nM, and 0.3 nM. On the other hand, betahistine exhibits full agonist activity, with an EC50 value of 0.1 μM in CHO (rH3(445)R), and inhibits cAMP production at concentrations higher than 10 nM [2].
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| ln Vivo |
Telemethylhistamine (t-MeHA) levels are raised by acute betahistine treatment (i.p. or oral; 0.1–30 mg/kg; single dose), with an ED50 of 0.4 mg/kg, indicating a reverse agonistic effect. Furthermore, upon acute oral treatment, male Swiss rats showed elevated t-MeHA levels, with an ED50 of 2 mg/kg [2]. In the paw tissue of CIA mice, betahistine (orally given; 1 and 5 mg/kg; once daily for 3 weeks) decreases the amount of pro-inflammatory cytokines and lessens the severity of arthritis [3].
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| Animal Protocol |
Animal/Disease Models: Collagen-induced arthritis (CIA) DBA/1 male mouse model [3]
Doses: 1 mg/kg; 5 mg/kg Route of Administration: oral; 21 days Results from day 21 to day 42 after CIA induction: Improves CIA in mice by reducing joint destruction. |
| 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.
[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. [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. |
| Molecular Formula |
C8H12N2
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|---|---|
| Molecular Weight |
136.19428
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| CAS # |
5638-76-6
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| Related CAS # |
Betahistine dihydrochloride;5579-84-0;Betahistine mesylate;54856-23-4
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| SMILES |
CNCCC1=NC=CC=C1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~100 mg/mL (~734.27 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (18.36 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 (18.36 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 (18.36 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 | 7.3427 mL | 36.7134 mL | 73.4268 mL | |
| 5 mM | 1.4685 mL | 7.3427 mL | 14.6854 mL | |
| 10 mM | 0.7343 mL | 3.6713 mL | 7.3427 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.
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