Benfotiamine

Catalog No.S4798 Synonyms: S-Benzoylthiamine O-monophosphate, Benzoylthiamine monophosphate

Benfotiamine Chemical Structure

Molecular Weight(MW): 466.45

Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2.

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Biological Activity

Description Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2.
In vitro

Benfotiamine improves the expression of endothelial cell markers in EPCs, restores eNOS levels, and recovers the ability of EPCs to participate in angiogenic processes. It is able to dampen glucose toxicity effects on endothelial progenitors[1]. Benfotiamine possesses antitumor activity against leukemia cells. In a panel of nine myeloid leukemia cell lines benfotiamine impairs the viability of HL-60, NB4, K562 and KG1 cells and also inhibits the growing of primary leukemic blasts. The antitumor activity of benfotiamine is not mediated by apoptosis, necrosis or autophagy, but rather occurs though paraptosis cell death induction. Benfotiamine inhibits the activity of constitutively active ERK1/2 and concomitantly increases the phosphorylation of JNK1/2 kinase in leukemic cells. In addition, benfotiamine induces the down regulation of the cell cycle regulator CDK3 which results in G1 cell cycle arrest in the sensitive leukemic cells[2].

In vivo Benfotiamine might exert vascular and renal benefits by modulating mechanisms independent or downstream of ROS formation. Benfotiamine aids the post-ischaemic healing of diabetic animals via PKB/Akt-mediated potentiation of angiogenesis and inhibition of apoptosis[3].

Protocol

Cell Research:[2]
+ Expand
  • Cell lines: leukemia cells (HL60, AML 1, NB4 cells)
  • Concentrations: 50 μM
  • Incubation Time: 24, 48, 72, 96 h
  • Method: Cell viability is assessed using a colorimetric MTT metabolic activity assay.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: diabetic animal model induced by STZ (male CD1 mice)
  • Formulation: 1 mmol/l HCl
  • Dosages: 80 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.01 mg/mL (0.02 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 466.45
Formula

C19H23N4O6PS

CAS No. 22457-89-2
Storage powder
in solvent
Synonyms S-Benzoylthiamine O-monophosphate, Benzoylthiamine monophosphate

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02772926 Completed Type 2 Diabetes Mellitus Universidad de Guanajuato October 2015 Not Applicable
NCT02772926 Completed Type 2 Diabetes Mellitus Universidad de Guanajuato October 2015 Not Applicable
NCT02292238 Active not recruiting Alzheimer''s Disease Burke Medical Research Institute|Burke Rehabilitation Hospital|Columbia University|National Institute on Aging (NIA)|Alzheimer’s Drug Discovery Foundation|Montefiore-Albert Einstein College of Medicine November 2014 Phase 2
NCT02292238 Active not recruiting Alzheimer''s Disease Burke Medical Research Institute|Burke Rehabilitation Hospital|Columbia University|National Institute on Aging (NIA)|Alzheimer’s Drug Discovery Foundation|Montefiore-Albert Einstein College of Medicine November 2014 Phase 2
NCT01868191 Unknown status Diabetic Neuropathies Diabetes Schwerpunktpraxis|Woerwag Pharma GmbH & Co. KG July 2013 Phase 3
NCT01868191 Unknown status Diabetic Neuropathies Diabetes Schwerpunktpraxis|Woerwag Pharma GmbH & Co. KG July 2013 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID