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Tolbutamide

Cat. No. M3077
Tolbutamide Structure
Synonym:

HLS 831

Size Price Availability Quantity
100mg USD 30  USD30 In stock
500mg USD 45  USD45 In stock
1g USD 55  USD55 In stock
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Quality Control & Documentation
Biological Activity

Tolbutamide is used along with diet and exercise, and sometimes with other medications, to treat type 2 diabetes Tolbutamide belongs to a class of medications called sulfonylureas. Tolbutamide lowers blood sugar by causing the pancreas to produce insulin (a natural substance that is needed to break down sugar in the body) and helping the body use insulin efficiently. This medication will only help lower blood sugar in people whose bodies produce insulin naturally. Tolbutamide is not used to treat type 1 diabetes (condition in which the body does not produce insulin and, therefore, cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition that may occur if high blood sugar is not treated). Tolbutamide inhibits both the basal and the cyclic AMP-stimulated protein kinase activities and the IC50 of Tolbutamide is 4 mM, and inhibits glucagon-induced phosphorylation of the bifunctional enzyme protein in a dose-dependent manner. Tolbutamide treatment significantly increases the binding of insulin to isolated adipocytes. The effect is associated with an enhanced response to insulin of the adipose tissue, since the fat cells obtained from animals treated with Tolbutamide convert significantly more glucose to lipids in the presence of insulin than those obtained from the control group .

Protocol (for reference only)
Cell Experiment
Cell lines C6 glioma cells
Preparation method Before each experiment, incubating C6 glioma cells in serum-free DMEM at 37 °C for at least 24 hours . Tolbutamide (400 μM) is incubated for 24 hours in serum-free medium. Incubations are performed at 37 °C in an atmosphere of 95% air/5% CO2 with 90–95% humidity
Concentrations 400 μM
Incubation time 24 hours
Animal Experiment
Animal models Male albino Wistar rats (200-300 g)
Formulation Tolbutamide is given as powder and mixed with food.
Dosages 450 mg/kg
Administration Tolbutamide is administered orally for 7 days.
Chemical Information
Molecular Weight 270.35
Formula C12H18N2O3S
CAS Number 64-77-7
Solubility (25°C) DMSO 42 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rosa Sanchez-Alvarez, et al. Glia. Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up-regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation

[2] H Ayame, et al. Am J Physiol. Tolbutamide inhibits glucagon-induced phosphorylation of 6PF-2-K/Fru-2,6-P2ase in rat hepatocytes

[3] H G Joost, et al. Biochem Pharmacol. Effects of tolbutamide on insulin binding to isolated fat cells of the rat

[4] H L Wray, et al. Biochem Biophys Res Commun. Adenosine 3', 5'-monophosphate-dependent protein kinase in adipose tissue: inhibition by tolbutamide

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Keywords: Tolbutamide, HLS 831 supplier, Potassium Channel, inhibitors, activators


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