For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug.<br>Target: Potassium Channel<br>Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). Tolbutamide act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Tolbutamide belongs to a class of medications called sulfonylureas. Tolbutamide inhibits both the basal and the cyclic AMP-stimulated protein kinase activities and the IC50 of Tolbutamide is 4 mM. Similar Tolbutamide concentrations are required for half maximal inhibition of in vitro lipolysis induced by hormones (norepinephrine and ACTH) or by dibutyryl cyclic AMP plus theophylline. Tolbutamide also inhibits both soluble and membrane-bound protein kinase from canine heart. The Tolbutamide inhibition of adipose tissue cyclic AMP-dependent protein kinase is one possible explanation for the antilipolytic effects of this drug [1]. Tolbutamide inhibits C6-glioma cell proliferation by increasing Cx43, which correlates with a reduction in pRb phosphorylation due to the up-regulation of the Cdk inhibitors p21 and p27 [2].<br></p>
| Catalog Number | I004440 |
| CAS Number | 64-77-7 |
| Synonyms | 1-butyl-3-(4-methylphenyl)sulfonylurea |
| Molecular Formula | C12H18N2O3S |
| Purity | ≥95% |
| Target | Potassium Channel |
| Solubility | DMSO: ≥ 34 mg/mL |
| Storage | 3 years -20C powder |
| InChIKey | JLRGJRBPOGGCBT-UHFFFAOYSA-N |
| Reference | </br>1:Effect of Temperature on Tolbutamide Binding to Glycated Serum Albumin. Szkudlarek A, Pentak D, Ploch A, Pożycka J, Maciążek-Jurczyk M.Molecules. 2017 Mar 31;22(4). pii: E569. doi: 10.3390/molecules22040569. PMID: 28362348 Free Article</br>2:Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and CYP Enzyme Substrates Sildenafil, Amlodipine, Tolbutamide, and Repaglinide. Gillen M, Yang C, Wilson D, Valdez S, Lee C, Kerr B, Shen Z.Clin Pharmacol Drug Dev. 2017 Jan 9. doi: 10.1002/cpdd.324. [Epub ahead of print] PMID: 28067999 </br>3:Altered tolbutamide pharmacokinetics by a decrease in hepatic expression of CYP2C6/11 in rats pretreated with 5-fluorouracil. Fukuno S, Nagai K, Kasahara K, Mizobata Y, Omotani S, Hatsuda Y, Myotoku M, Konishi H.Xenobiotica. 2017 Jan 31:1-7. doi: 10.1080/00498254.2017.1278808. [Epub ahead of print] PMID: 28051340 </br>4:Thermodynamic Stability Analysis of Tolbutamide Polymorphs and Solubility in Organic Solvents. Svärd M, Valavi M, Khamar D, Kuhs M, Rasmuson ÅC.J Pharm Sci. 2016 Jun;105(6):1901-6. doi: 10.1016/j.xphs.2016.03.021. PMID: 27238487 </br>5:Subtle structural changes in the Asp251Gly/Gln307His P450 BM3 mutant responsible for new activity toward diclofenac, tolbutamide and ibuprofen. Di Nardo G, Dell/’Angelo V, Catucci G, Sadeghi SJ, Gilardi G.Arch Biochem Biophys. 2016 Jul 15;602:106-15. doi: 10.1016/j.abb.2015.12.005. Epub 2015 Dec 21. PMID: 26718083 </br>6:Application of a New Dynamic Model to Predict the In Vitro Intrinsic Clearance of Tolbutamide Using Rat Microsomes Encapsulated in a Fab Hydrogel. Zhou N, Zheng Y, Xing J, Yang H, Chen H, Xiang X, Liu J, Tong S, Zhu B, Cai W.Drug Metab Dispos. 2016 Jan;44(1):40-9. doi: 10.1124/dmd.115.066092. Epub 2015 Oct 14. PMID: 26467766 Free Article</br>7:Novel Marmoset Cytochrome P450 2C19 in Livers Efficiently Metabolizes Human P450 2C9 and 2C19 Substrates, S-Warfarin, Tolbutamide, Flurbiprofen, and Omeprazole. Uehara S, Uno Y, Inoue T, Kawano M, Shimizu M, Toda A, Utoh M, Sasaki E, Yamazaki H.Drug Metab Dispos. 2015 Oct;43(10):1408-16. doi: 10.1124/dmd.115.066100. Epub 2015 Jul 30. PMID: 26228688 Free Article</br>8:Prenatal tolbutamide treatment alters plasma glucose and insulin concentrations and negatively affects the postnatal performance of chickens. Franssens L, Lesuisse J, Wang Y, De Ketelaere B, Willems E, Koppenol A, Guo X, Buyse J, Decuypere E, Everaert N.Domest Anim Endocrinol. 2015 Jul;52:35-42. doi: 10.1016/j.domaniend.2015.01.004. Epub 2015 Jan 28. PMID: 25727896 </br>9:Simultaneous determination of bupropion, metroprolol, midazolam, phenacetin, omeprazole and tolbutamide in rat plasma by UPLC-MS/MS and its application to cytochrome P450 activity study in rats. Ma J, Wang S, Zhang M, Zhang Q, Zhou Y, Lin C, Lin G, Wang X.Biomed Chromatogr. 2015 Aug;29(8):1203-12. doi: 10.1002/bmc.3409. Epub 2015 Jan 13. PMID: 25582505 </br>10:Evaluation of CYP2C9 Activity in Rats: Use of Tolbutamide Alone and in Combined with Bupropion. Qiu X, Song J, Yuan H, Hou Y, Pan X, Xu RA.Iran J Pharm Res. 2014 Spring;13(2):635-9. PMID: 25237359 Free PMC Article |
