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Tolbutamide

Catalog No. T1054   CAS 64-77-7
Synonyms: HLS 831

Tolbutamide (HLS 831) is a sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.

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Tolbutamide Chemical Structure
Tolbutamide, CAS 64-77-7
Pack Size Availability Price/USD Quantity
500 mg In stock $ 41.00
1 g In stock $ 59.00
1 mL * 10 mM (in DMSO) In stock $ 45.00
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Purity: 99.65%
Purity: 98.37%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tolbutamide (HLS 831) is a sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.
Targets&IC50 cyclic AMP-stimulated protein kinase:4 mM
In vitro Daily treatment of cells with 450 mg/kg of Tolbutamide for seven consecutive days significantly increases the binding of insulin to adipocytes. The binding curve suggests an increase in the number of receptor sites rather than an increased affinity. This effect is associated with an enhanced insulin response in adipose tissue. Compared to the control group, adipocytes from Tolbutamide-treated animals show a notable increase in the conversion of glucose to fat in the presence of insulin. While low doses of Tolbutamide can elicit a metabolic effect by stimulating insulin secretion, they do not augment the number of insulin binding sites. An increase in insulin binding sites occurs only in the presence of high doses of Tolbutamide, which, at such levels, reduces overall insulin, including its pancreatic secretion and serum levels.
In vivo Tolbutamide is effective only in patients who can normally produce insulin, as it helps to lower blood glucose levels. The compound inhibits the activity of both basal protein kinase and cyclic AMP-activated protein kinase, with an IC50 concentration of 4 mM. It dose-dependently inhibits the phosphorylation of bifunctional proteins induced by glucagon. In the presence of 10(-9) M glucagon, adding 2 mM Tolbutamide reduces the activity of 6-phosphofructokinase and enhances the activity of fructose-2,6-bisphosphatase. Additionally, Tolbutamide inhibits the activity of free and membrane-bound proteases in canine cardiac tissue. Its inhibitory effect on cyclic AMP-dependent protein kinase activity in adipose tissue may account for its antilipolytic action. Tolbutamide also inhibits the proliferation of C6 glioma cells by increasing the concentration of Cx43, which is associated with reduced phosphorylation of pRb due to upregulation of the cyclin-dependent kinase inhibitors p21 and p27.
Kinase Assay cAMP kinase assay: Diced epididymal fat pads from fed Wistar rats (175-225 gm) are obtained after decapitation and incubated at 37 °C for two hours in Krebs-bicarbonate buffer containing 1.27 mM CaCl2. When added, Tolbutamide is present only during the incubation. After incubation fat pads are rinsed and sonicated in cold Krebs-bicarbonate buffer. The aqueous supematants from centrifugation at 50,000 × g for 30 minutes at 4 °C contained 0.75 to 1.25 mg protein per mL and are assayed for cyclic AMP-stimulated protein kinase activity. The assay is performed in 0.2 mL with these additions, 10 μmoles sodium glycerofiosphate pH 7.0, 2 μmoles sodium fluoride, 0.4 μmoles theophylline, 0.1 μmoles ethylene glyool bis (β-aminoethyl ether)-N, N'-tetraaoetic acid, 3 μmoles magnesium chloride, 0.3 mg mixed histone, 2 nmoles (γ- 32P) ATP, 1 nmoles cyclic AMP when indicated, and 0.05 ml of supernatant.
Cell Research C6 glioma cells are incubated in serum-free DMEM at 37 °C for at least 24 hours before each experiment. 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. (Only for Reference)
Synonyms HLS 831
Molecular Weight 270.35
Formula C12H18N2O3S
CAS No. 64-77-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (184.9 mM)

Ethanol: 50 mg/mL (184.9 mM)

TargetMolReferences and Literature

1. Wray HL, et al, Biochem Biophys Res Commun. 1973, 53(1), 291-294. 2. Sanchez-Alvarez R, et al, Glia, 2006, 54(2), 125-134. 3. Schwanstecher C, et al, Mol Pharmacol, 1992, 41(3), 480-486. 4. Avame H, et al, Am J Physiol, 1995, 268(3 Pt 1), 392-396. 5. Joost HG, et al, Biochem Pharmacol, 1982, 31(7), 1227-1231.

TargetMolCitations

1. Guo J, Xu Y, Chen L J, et al. Gut Microbiota and Host Cyp450s Co-contribute to Pharmacokinetic Variability in Mice With Non-Alcoholic Steatohepatitis: Vary From Drug to Drug. Journal of Advanced Research. 2021

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library NO PAINS Compound Library Drug Repurposing Compound Library Ion Channel Inhibitor Library Anti-Cancer Compound Library Anti-Metabolism Disease Compound Library Drug-Fragment Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Tolbutamide 64-77-7 Autophagy Membrane transporter/Ion channel Potassium Channel inhibit Inhibitor HLS-831 KcsA HLS 831 HLS831 inhibitor

 

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