| Size | Price | Stock | Qty |
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| 1g |
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| 10g |
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| 25g | |||
| Other Sizes |
| Targets |
Sulbutiamine does not have a specific pharmacological target; it acts as a thiamine (vitamin B1) prodrug, increasing thiamine levels in the brain. Thiamine is an essential cofactor for several enzymes involved in carbohydrate metabolism, including pyruvate dehydrogenase, α-ketoglutarate dehydrogenase, and transketolase. By increasing thiamine levels, sulbutiamine enhances energy metabolism in the brain.
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| ln Vitro |
When hippocampal CA1 pyramidal neurons are exposed to glucose hypoxia, sulbutiamine has neuroprotective effects on them. In a concentration-dependent manner, sulbutiamine improves electrophysiological characteristics like excitatory synaptic transmission and intrinsic neuronal membrane input resistance [1]. Serum deprivation-induced apoptosis is attenuated by sulbutiamine, which also dose-dependently increases GSH and GST activity. Furthermore, cleaved caspase-3 and AIF expression can also be decreased by sulbutiamine [2].
In vitro, sulbutiamine is an antioxidant that acts by inhibiting oxidative stress-induced retinal ganglion cell death. It increases the levels of thiamine and thiamine triphosphate in the brain. Its effects on cellular metabolism and oxidative stress are being studied. |
| ln Vivo |
In vivo, sulbutiamine is used to treat symptoms of weakness or fatigue. It is also sold as a dietary supplement to enhance cognitive function, improve mood, and increase energy levels. It is marketed under the brand name Arcalion.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not typically performed for sulbutiamine as it is a thiamine derivative, not a direct enzyme inhibitor. Its activity is assessed by measuring its effects on cellular metabolism and thiamine levels in cell-based assays.
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| Cell Assay |
For in vitro cell-based assays, sulbutiamine is dissolved in DMSO and applied to cultured cells at concentrations ranging from 1-100 µM. The effects on cell viability, oxidative stress, and energy metabolism are assessed after 24-72 hours of treatment.
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| Animal Protocol |
In vivo animal studies for sulbutiamine are typically conducted in rodent models of fatigue or cognitive impairment. Sulbutiamine is administered orally or intraperitoneally at doses ranging from 1-100 mg/kg. Efficacy is evaluated by measuring physical performance, cognitive function, and biochemical markers of energy metabolism.
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| ADME/Pharmacokinetics |
Sulbutiamine has a molecular formula of C₃₂H₄₆N₈O₆S₂ and a molecular weight of 702.88 g/mol. It is a highly lipophilic compound. It is soluble in DMSO and is typically stored as a powder at 2-8°C.
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| Toxicity/Toxicokinetics |
Sulbutiamine is considered to have a manageable toxicity profile. Common side effects may include gastrointestinal disturbances, headache, and skin reactions. No significant hepatotoxicity or nephrotoxicity has been reported.
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| References |
[1]. Kwag J, et al. Evidence for neuroprotective effect of sulbutiamine against oxygen-glucose deprivation in rat hippocampal CA1 pyramidal neurons. Biol Pharm Bull. 2011;34(11):1759-64.
[2]. Kang KD, et al. Sulbutiamine counteracts trophic factor deprivation induced apoptotic cell death in transformed retinal ganglion cells. Neurochem Res. 2010 Nov;35(11):1828-39. |
| Additional Infomation |
Bisibuthiamine is an aminopyrimidine compound. Subutyramine is a synthetic derivative of thiamine (vitamin B1), marketed as Arcalion, and is a dimer formed from two modified thiamine molecules. It is highly lipophilic, thus crossing the blood-brain barrier more easily than other thiamine derivatives. Although its clinical efficacy is not yet fully established, subutyramine has been used to treat fatigue. Among other uses, subutyramine has been used to improve erectile dysfunction and reduce psychomotor inhibition, and there is evidence that it has a regulatory effect on dopaminergic and glutamatergic cortical transmission. Long-term use of this drug has been shown to improve long-term memory formation in mice.
Sulbutiamine is a synthetic derivative of thiamine (vitamin B1) used for the treatment of asthenia and as a dietary supplement. It is also known as bisibuthiamine. Sulbutiamine is approved for clinical use in some countries. It is supplied by various pharmaceutical and research chemical suppliers for human and research use. |
| Molecular Formula |
C32H46N8O6S2
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|---|---|
| Molecular Weight |
702.89
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| Exact Mass |
702.2982
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| CAS # |
3286-46-2
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| PubChem CID |
3002120
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
726.0±60.0 °C at 760 mmHg
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| Melting Point |
140.5-141.5 °C
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| Flash Point |
392.9±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.702
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| LogP |
7.51
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
48
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C/C(N(C=O)CC1=CN=C(C)N=C1N)=C(CCOC(C(C)C)=O)/SS/C(CCOC(C(C)C)=O)=C(C)\N(C=O)CC2=CN=C(C)N=C2N
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| InChi Key |
CKHJPWQVLKHBIH-ZDSKVHJSSA-N
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| InChi Code |
InChI=1S/C32H46N8O6S2/c1-19(2)31(43)45-11-9-27(21(5)39(17-41)15-25-13-35-23(7)37-29(25)33)47-48-28(10-12-46-32(44)20(3)4)22(6)40(18-42)16-26-14-36-24(8)38-30(26)34/h13-14,17-20H,9-12,15-16H2,1-8H3,(H2,33,35,37)(H2,34,36,38)/b27-21-,28-22-
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| Chemical Name |
[(Z)-4-[(4-Amino-2-methylpyrimidin-5-yl)methyl-formylamino]-3-[[(Z)-2-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-5-(2-methylpropanoyloxy)pent-2-en-3-yl]disulfanyl]pent-3-enyl] 2-methylpropanoate
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| Synonyms |
Bisibutiamine VitaberinBisibuthiamine SulbutiamineArcalion
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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 |
| 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 (~142.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.56 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 (3.56 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4227 mL | 7.1135 mL | 14.2270 mL | |
| 5 mM | 0.2845 mL | 1.4227 mL | 2.8454 mL | |
| 10 mM | 0.1423 mL | 0.7113 mL | 1.4227 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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