| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
| ln Vitro |
In a preliminary study, Fursultiamine in combination with glucosamine hydrochloride and/or chondroitin sulfate showed no detectable additive beneficial effects on cellular metabolism of bovine nasal cartilage or human articular chondrocytes in vitro. [1]
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| ln Vivo |
In a rabbit partial medial meniscectomy model of osteoarthritis, oral administration of Fursultiamine alone at 100 mg/kg for 8 weeks had no effect on the severity of macroscopic or histologic cartilage lesions, nor on MMP-1 positive cell scores compared to placebo-treated OA rabbits. However, when combined with glucosamine hydrochloride (1000 mg/kg) and chondroitin sulfate (800 mg/kg), the triple combination significantly reduced macroscopic lesion grade (by 40%) and surface area (by 39%), histologic score (by 44%), and MMP-1 positive chondrocytes (by 42%) compared to placebo. [1]
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| Animal Protocol |
Male Japanese White rabbits (13-week-old, 2.5-2.9 kg) underwent partial medial meniscectomy of the right knee joint (day 0) under anesthesia. Treatment was initiated on day 3 and continued for 8 weeks. Fursultiamine was dissolved in distilled water and administered via a gastric tube once daily at a dose of 100 mg/kg. For the combination study, glucosamine hydrochloride (1000 mg/kg) and sodium chondroitin sulfate (800 mg/kg) were co-administered. Placebo control received distilled water. Another experiment evaluated Fursultiamine alone at the same dose. Rabbits were sacrificed with sodium pentobarbital. Macroscopic grading of tibial plateau cartilage (depth score 0-4, area measured by image analysis), histologic grading (Safranin O-fast green staining, Mankin scale 0-12), and immunohistochemistry for MMP-1 (mouse monoclonal antibody, percent positive chondrocytes) were performed. [1]
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| ADME/Pharmacokinetics |
Oral administration of Fursultiamine at 50 mg/kg in rabbits rapidly caused a sufficient increase in blood total thiamine level reaching up to 4 pg/mL, which is about 10 times higher than that in humans at its regular dose (100 mg/min). During absorption, the S-S bond of Fursultiamine is broken to generate thiamine. [1]
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| Toxicity/Toxicokinetics |
No clinical signs of drug toxicity were noted in any treatment group. A slight but significant decrease in body weight gain was observed in rabbits treated with GH+CS+Fursultiamine compared to placebo control (p<0.05 at day 56), but not in rabbits treated with Fursultiamine alone. [1]
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| References | |
| Additional Infomation |
Fursultiamine belongs to the pyrimidine class of compounds. This compound is used to treat thiamine deficiency. It has also been used to treat various non-deficiency diseases, but its effectiveness has not been proven. Fursultiamine is a vitamin B1 derivative. It is a nutritional supplement and vitamin B1 derivative with potential anti-tumor activity. Oral administration of Fursultiamine inhibits the expression of octamer-binding transcription factor 4 (OCT-4), SRY (sex-determining region Y)-box 2 (SOX-2), and Nanog homeobox (NANOG) in cancer stem cells (CSCs). This may inhibit CSC proliferation, thereby preventing tumor cell growth. Furthermore, Fursultiamine inhibits the expression of ATP-binding cassette (ABC) transporter subfamily B member 1 (ABCB1) and subfamily G member 2 (ABCG2) in cancer stem cells (CSCs), which may eliminate CSC resistance to chemotherapy and radiotherapy. CSCs promote tumor development, progression, and metastasis; they play a key role in cancer recurrence and resistance to chemotherapy and radiotherapy. This compound is used to treat thiamine deficiency. It has also been recommended for the treatment of several non-deficiency diseases, but its effectiveness has not been proven.
Fursultiamine is a vitamin B1 derivative. It may provide preferential conditions for collagen synthesis via regulation of ascorbic acid biosynthesis, as thiamine deficiency has been reported to reduce collagen synthesis. It also enhances thermogenesis together with noradrenaline and adrenaline secretion in rats. The combined treatment with glucosamine (which may affect energy balance via the hexosamine biosynthesis pathway) and Fursultiamine may increase energy expenditure and decrease energy intake, leading to changes in body weight gain. B vitamins have been reported to induce antinociceptive effects and increase the analgesic effect of NSAIDs. [1] |
| Molecular Formula |
C17H26N4O3S2
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|---|---|
| Molecular Weight |
398.5433
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| Exact Mass |
398.144
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| CAS # |
804-30-8
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| Related CAS # |
67-03-8 ( Thiamine HCl; Vitamin B1 HCl salt); 16816-67-4 ( Pantethine, a derivative of vitamin B5); 29883-15-6 (Vitamin B17 derivative); 22457-89-2 (synthetic vitamin B1; BRN-0771326; BTMP; CB-8088; Berdi; Betivina; Biotamin; Benfotiamine; S-benzoylthiamine O-monophosphate); 59-30-3 (Folic acid); 13870-90-1 [Coenzyme B12 (adenosylcobalamin; AdoCbl)]; 68-19-9 (vitamin B 12 related); 13422-55-4 (Mecobalamin, an analog of Vitamin B12); 80037-86-1 (Succinylacetone pyrrole, an inhibitor of vitamin B12 biosynthesis)
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| PubChem CID |
3002119
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
652.3±55.0 °C at 760 mmHg
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| Melting Point |
130-136ºC (decompos.)
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| Flash Point |
348.3±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.626
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| LogP |
2.35
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
26
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| Complexity |
481
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=CN(CC1C(N)=NC(C)=NC=1)C(C)=C(CCO)SSCC1CCCO1
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| InChi Key |
JTLXCMOFVBXEKD-FOWTUZBSSA-N
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| InChi Code |
InChI=1S/C17H26N4O3S2/c1-12(16(5-6-22)26-25-10-15-4-3-7-24-15)21(11-23)9-14-8-19-13(2)20-17(14)18/h8,11,15,22H,3-7,9-10H2,1-2H3,(H2,18,19,20)/b16-12+
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| Chemical Name |
(E)-N-((4-amino-2-methylpyrimidin-5-yl)methyl)-N-(5-hydroxy-3-(((tetrahydrofuran-2-yl)methyl)disulfanyl)pent-2-en-2-yl)formamide
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| Synonyms |
Fursultiamine; Judolor; Linamin; EINECS 212-357-1; Tetrahydrofurfuryl thiamine disulfide; TTFD; Adventan, Alinamin-F, Benlipoid, Bevitol Lipophil, Judolor, Lipothiamin
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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 : ~106.7 mg/mL (~267.73 mM)
H2O : ≥ 6.67 mg/mL (~16.74 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 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 (6.27 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 (6.27 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 | 2.5092 mL | 12.5458 mL | 25.0916 mL | |
| 5 mM | 0.5018 mL | 2.5092 mL | 5.0183 mL | |
| 10 mM | 0.2509 mL | 1.2546 mL | 2.5092 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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