| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
AMP-activated protein kinase (AMPK) / peroxisome proliferator-activated receptor-γ coactivator-1β (PGC-1β) / nuclear respiratory factor-1 (NRF-1) axis in mitochondria of hepatocytes in fish (Megalobrama amblycephala). [1]
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| ln Vivo |
Dietary supplementation with benfotiamine at 1.425 mg/kg for 12 weeks improved the growth performance (increased final weight, weight gain rate, specific growth rate) of juvenile blunt snout bream (Megalobrama amblycephala) fed a high-carbohydrate (HC, 43% carbohydrate) diet compared to fish fed the HC diet alone.
Dietary benfotiamine supplementation at 1.425 mg/kg ameliorated the metabolic disturbances induced by the HC diet. It significantly increased plasma insulin levels and tissue (liver, muscle, adipose) glycogen and lipid contents, while it significantly decreased plasma glucose, glycated serum protein (GSP), and advanced glycation end products (AGEs) levels in the fish. Benfotiamine supplementation (1.425 mg/kg) increased the phosphorylated AMPKα to total AMPKα protein ratio and the protein expression of PGC-1β in the fish liver. Benfotiamine supplementation (1.425 mg/kg) upregulated the hepatic mRNA transcriptions of genes involved in mitochondrial biogenesis and fusion, including AMPKα-2, PGC-1β, NRF-1, mitochondrial transcription factor A (TFAM), mitofusin-1 (Mfn-1), and optic atrophy-1 (Opa-1). Conversely, it downregulated the transcriptions of genes involved in mitochondrial fission, such as dynamin-related protein-1 (Drp-1), fission-1 (Fis-1), and mitochondrial fission factor (Mff). Benfotiamine supplementation (1.425 mg/kg) increased the activities of mitochondrial respiratory chain complexes I, II, III, IV, and V in the fish liver. Benfotiamine supplementation (1.425 mg/kg) increased the hepatic mRNA transcriptions of mitochondrial function-related genes, including cytochrome b (CYT-b), cytochrome c oxidase-2 (COX-2), and ATP synthase-6 (ATP-6). The optimal dietary dose for improving growth and mitochondrial function in this fish model under HC diet conditions was 1.425 mg/kg. Higher doses (2.85 and 5.7 mg/kg) did not provide additional benefits and even impaired growth at the highest dose. [1] |
| Enzyme Assay |
Mitochondrial respiratory chain complex activities were measured in isolated liver mitochondria. Briefly, liver samples were homogenized in a cold extraction medium containing KH2PO4, sucrose, and EDTA. The homogenate was centrifuged at low speed, and the supernatant was retained. The mitochondrial fraction was obtained by further centrifugation. The sediment (mitochondrial pellet) was washed, resuspended, and stored. Mitochondrial protein concentration was determined. The activities of complexes I, II, III, IV, and V were measured using established spectrophotometric or other biochemical methods. Complex I-III activity was measured according to a referenced method. Complex IV and V activities were analyzed using another referenced method. The activities were expressed as nanomoles per minute per milligram of protein. [1]
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| Animal Protocol |
Three hundred sixty juvenile blunt snout bream (average initial weight: 45.25 ± 0.34 g) were randomly distributed into 24 tanks (15 fish per tank). The fish were fed one of six experimental diets for 12 weeks. The diets included: a control diet (30% carbohydrate, C), a high-carbohydrate diet (43% carbohydrate, HC), and the HC diet supplemented with four different levels of benfotiamine: 0.7125 (HCB1), 1.425 (HCB2), 2.85 (HCB3), and 5.7 (HCB4) mg per kg of diet. The benfotiamine was mixed into the diet during formulation. Fish were fed to visual satiation three times daily (07:00, 12:00, and 17:00). Water temperature was maintained at 27.4 ± 0.6°C, with a photoperiod of 12h light:12h dark, and dissolved oxygen above 5.0 mg/L. After the 12-week feeding period, fish were fasted for 24 hours, anesthetized, and blood and tissues (liver, muscle, adipose) were collected for analysis. [1]
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| Toxicity/Toxicokinetics |
Adding 5.7 mg/kg of fenprophane (the highest tested dose) to the feed significantly reduced the final body weight, weight gain rate, and specific growth rate of the fish, suggesting that this high dose may have an inhibitory effect on growth under the experimental conditions compared to the optimal dose group. No deaths were observed in any of the 12-week trials. The study did not provide specific toxicity data, such as LD50, organ histopathology, or plasma biochemical markers of organ damage. [1]
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| References |
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| Additional Infomation |
Benfotiamine is a thioester, a synthetic analog of thiamine, obtained through acylation and O-phosphorylation of the thiazole ring. It has functions as an immune adjuvant, nutritional supplement, antioxidant, provitamin B1, and protectant. It is an aminopyrimidine, belonging to the formamide class, organophosphates, and thioesters. Its function is related to thiamine (1+). Benfotiamine has been investigated for the treatment and prevention of diabetic nephropathy and type 2 diabetes. See also: Benfotiamine (note moved to). Benfotiamine can be used as a dietary supplement to treat diabetic complications. It can improve glucose homeostasis by blocking three major pathways associated with hyperglycemic damage: the hexosamine pathway, the advanced glycation end products (AGEs) formation pathway, and the diacylglycerol (DAG)-protein kinase C pathway. Benfotiamine can enhance the activity of dehydrogenase complexes by increasing intracellular thiamine diphosphate (TPP) levels, thereby increasing glucose oxidation in mitochondria.
Benzothiamethoxam can alleviate stress caused by excessive production of superoxide anions in the mitochondrial electron transport chain. In this fish study, Benzothiamethoxam improved mitochondrial biosynthesis and function in the liver by activating the AMPK/PGC-1β/NRF-1 axis, upregulating mitochondrial fusion genes, enhancing the activity of mitochondrial respiratory chain complexes, and inhibiting mitochondrial fission. [1] |
| Molecular Formula |
C19H23N4O6PS
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|---|---|
| Molecular Weight |
466.4488
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| Exact Mass |
466.107
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| CAS # |
22457-89-2
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| Related CAS # |
147317-17-7 (semihydrate);22457-89-2 (free acid);
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| PubChem CID |
3032771
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
745.1±70.0 °C at 760 mmHg
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| Melting Point |
165ºC
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| Flash Point |
404.4±35.7 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.645
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| LogP |
1.81
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
31
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| Complexity |
697
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NC=C(C(=N1)N)CN(C=O)/C(=C(/CCOP(=O)(O)O)\SC(=O)C2=CC=CC=C2)/C
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| InChi Key |
BTNNPSLJPBRMLZ-LGMDPLHJSA-N
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| InChi Code |
InChI=1S/C19H23N4O6PS/c1-13(23(12-24)11-16-10-21-14(2)22-18(16)20)17(8-9-29-30(26,27)28)31-19(25)15-6-4-3-5-7-15/h3-7,10,12H,8-9,11H2,1-2H3,(H2,20,21,22)(H2,26,27,28)/b17-13-
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| Chemical Name |
S-[(Z)-2-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-5-phosphonooxypent-2-en-3-yl] benzenecarbothioate
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| Synonyms |
CB 8088 Berdi Betivina BiotaminBRN-0771326 BTMP CB-8088 CB8088 Benfotiamine S-benzoylthiamine O-monophosphate
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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 : ≥ 50 mg/mL (~107.19 mM)
H2O : ~0.67 mg/mL (~1.44 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (6.43 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 30.0 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: ≥ 3 mg/mL (6.43 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 30.0 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: ≥ 3 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 3.12 mg/mL (6.69 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1439 mL | 10.7193 mL | 21.4385 mL | |
| 5 mM | 0.4288 mL | 2.1439 mL | 4.2877 mL | |
| 10 mM | 0.2144 mL | 1.0719 mL | 2.1439 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02292238 | COMPLETEDWITH RESULTS | Drug: Benfotiamine | Alzheimer's Disease | Burke Medical Research Institute | 2015-02-15 | Phase 2 |
| NCT01868191 | UNKNOWN STATUS | Drug: Benfotiamine Drug: Placebo for benfotiamine |
Diabetic Neuropathies | Diabetes Schwerpunktpraxis | 2013-07 | Phase 3 |
| NCT00565318 | COMPLETED | Drug: Benfotiamine Drug: Placebo |
Diabetic Nephropathy | University Medical Center Groningen | 2007-12 | Phase 4 |
| NCT00785460 | COMPLETED | Drug: Benfotiamine | Healthy Subjects | Ruhr University of Bochum | 2008-01 | Phase 3 |
| NCT03892707 | COMPLETEDWITH RESULTS | Drug: Exposure of interest (within routine clinical practice): Vitamin B complexes Milgamma® and Milgamma® compositum |
Acute Non-specific Low Back Pain | Woerwag Pharma LLC | 2018-12-15 |
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