Fursultiamine targets the same metabolic pathways as thiamine (vitamin B1). Thiamine is an essential cofactor for several enzymes involved in carbohydrate metabolism, including pyruvate dehydrogenase, alpha-ketoglutarate dehydrogenase, and transketolase. By providing a bioavailable source of thiamine, fursultiamine supports energy metabolism and neurological function.

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]
In vitro, Fursultiamine is converted to thiamine in cells and serves as a cofactor for thiamine-dependent enzymes. It supports cellular energy metabolism by facilitating the conversion of pyruvate to acetyl-CoA and the function of the Krebs cycle. It may also have antioxidant properties and support neuronal function.

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]
In vivo, Fursultiamine is used as a dietary supplement for the prevention and treatment of thiamine deficiency. It is more lipophilic than thiamine and is better absorbed from the gastrointestinal tract. It is used to support energy metabolism, neurological function, and cardiovascular health. It is available as an over-the-counter supplement.

In vitro enzyme assays for Fursultiamine involve measuring the activity of thiamine-dependent enzymes, such as transketolase or pyruvate dehydrogenase. Cells or tissue homogenates are incubated with fursultiamine or thiamine, and enzyme activity is measured spectrophotometrically. The compound's ability to restore enzyme activity in thiamine-deficient cells can be assessed.

In vitro cell-based assays for Fursultiamine are performed using cell lines that are thiamine-deficient or have impaired thiamine metabolism. Cells are cultured in appropriate media and treated with fursultiamine at various concentrations. Cell viability is measured by MTT assays. Thiamine-dependent enzyme activity is measured in cell lysates. The effects on cellular metabolism and oxidative stress can also be assessed.

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]
In vivo animal studies for Fursultiamine are conducted in models of thiamine deficiency. Animals are fed a thiamine-deficient diet, and fursultiamine is administered orally or via injection. The compound's ability to restore thiamine levels, enzyme activity, and physiological function is assessed. Parameters such as body weight, neurological function, and metabolic parameters are monitored.

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]
Fursultiamine is absorbed from the gastrointestinal tract and is converted to thiamine in the body. It is distributed to various tissues, including the brain, liver, and muscle. It is metabolized to thiamine and excreted primarily in urine. Its lipophilic nature enhances its bioavailability compared to thiamine.

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]
Fursultiamine is generally well-tolerated when used as a dietary supplement. High doses may cause mild gastrointestinal disturbances. It is not associated with significant toxicity. It is contraindicated in patients with known hypersensitivity to thiamine or fursultiamine. It is not intended for therapeutic use in the absence of thiamine deficiency.

Inflamm Res. 2005 Jun;54(6):249-55.

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.

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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]
Fursultiamine is a lipophilic, highly absorbable form of vitamin B1 (thiamine). It is used as a dietary supplement for the prevention and treatment of thiamine deficiency. Fursultiamine supports energy metabolism and neurological function. This product is for research and nutritional use.

C17H26N4O3S2

398.5433

398.144

804-30-8

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)

3002119

White to off-white solid powder

1.3±0.1 g/cm3

652.3±55.0 °C at 760 mmHg

130-136ºC (decompos.)

348.3±31.5 °C

0.0±2.1 mmHg at 25°C

1.626

2.35

2

8

9

26

481

0

O=CN(CC1C(N)=NC(C)=NC=1)C(C)=C(CCO)SSCC1CCCO1

JTLXCMOFVBXEKD-FOWTUZBSSA-N

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+

(E)-N-((4-amino-2-methylpyrimidin-5-yl)methyl)-N-(5-hydroxy-3-(((tetrahydrofuran-2-yl)methyl)disulfanyl)pent-2-en-2-yl)formamide

Fursultiamine; Judolor; Linamin; EINECS 212-357-1; Tetrahydrofurfuryl thiamine disulfide; TTFD; Adventan, Alinamin-F, Benlipoid, Bevitol Lipophil, Judolor, Lipothiamin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~106.7 mg/mL (~267.73 mM)
H2O : ≥ 6.67 mg/mL (~16.74 mM)

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.

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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.

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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.
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 corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)