| Size | Price | Stock | Qty |
|---|---|---|---|
| 10g |
|
||
| 25g |
|
||
| 50g |
|
||
| 100g |
|
||
| Other Sizes |
|
Sulbutiamine is a novel and potent antioxidant acting by inhibiting oxidative stress induced retinal ganglion cell death. It is a lipid soluble synthetic analogue of vitamin B1 that can be used for the treatment of asthenia.
| 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].
|
|---|---|
| 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.
Sulbutiamine is a synthetic derivative of thiamine (vitamin B1) under the market name Arcalion that is composed of two modified thiamine molecules to form a dimer. It is highly lipophilic, allowing it to cross the blood-brain barrier more easily than other thiamine derivatives. Although its clinical efficacy is not yet defined, sulbutiamine is used to treat asthenia. While its other uses include improvement of erectile dysfunction and reduction of psycho-behavioural inhibition, sulbutiamine showed evidence of modulatory effect on dopaminergic and glutamatergic cortical transmissions. The chronic administration of the drug has demonstrated to improve long term memory formation in mice. |
| Molecular Formula |
C32H46N8O6S2
|
|---|---|
| Molecular Weight |
702.89
|
| Exact Mass |
702.2982
|
| CAS # |
3286-46-2
|
| PubChem CID |
3002120
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
726.0±60.0 °C at 760 mmHg
|
| Melting Point |
140.5-141.5 °C
|
| Flash Point |
392.9±32.9 °C
|
| Vapour Pressure |
0.0±2.4 mmHg at 25°C
|
| Index of Refraction |
1.702
|
| LogP |
7.51
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
19
|
| Heavy Atom Count |
48
|
| Complexity |
1050
|
| Defined Atom Stereocenter Count |
0
|
| 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
|
| InChi Key |
CKHJPWQVLKHBIH-ZDSKVHJSSA-N
|
| 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-
|
| 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
|
| Synonyms |
Bisibutiamine VitaberinBisibuthiamine SulbutiamineArcalion
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~142.27 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
