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[CAS NO. 64-77-7] Tolbutamide
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-B0401 |
| Brand: | MCE |
| CAS: | 64-77-7 |
Overview
| MDL | MFCD00027169 |
|---|---|
| Molecular Weight | 270.35 |
| Molecular Formula | C12H18N2O3S |
| SMILES | O=S(C1=CC=C(C)C=C1)(NC(NCCCC)=O)=O |
2 Publications Citing Use of MCE
Summary
Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug. Target: Potassium Channel 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].
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01061112 | University of Minnesota|National Institute of General Medical Sciences (NIGMS) |
Healthy
|
December 2009 | |
| NCT03723395 | Seagen Inc. |
Drug-drug Interaction
|
September 17, 2018 | Phase 1 |
| NCT00930306 | AstraZeneca |
Chronic Pain
|
June 2009 | Phase 1 |
| NCT01185548 | Eli Lilly and Company |
Lymphoma|Advanced Cancer
|
July 2010 | Phase 1 |
| NCT01525628 | Boehringer Ingelheim |
Hepatitis C, Chronic
|
April 2012 | Phase 1 |
| NCT02211079 | Janssen Research & Development, LLC |
Healthy
|
September 2014 | Phase 1 |
| NCT05097716 | Pfizer |
Healthy Volunteers
|
November 2, 2021 | Phase 1 |
| NCT03457597 | Corcept Therapeutics |
Healthy
|
March 6, 2018 | Phase 1 |
| NCT01218620 | National Cancer Institute (NCI) |
Adult Solid Neoplasm
|
September 2010 | Phase 1 |
| NCT03291288 | Daiichi Sankyo, Inc. |
Drug Interaction Potential
|
February 26, 2018 | Phase 1 |
| NCT02182401 | Boehringer Ingelheim |
Healthy
|
July 2009 | Phase 1 |
| NCT03948243 | University of Illinois at Chicago|Oregon State University |
Food-drug Interaction
|
April 1, 2019 | Phase 1 |
| NCT02473627 | Daiichi Sankyo, Inc. |
Healthy
|
May 2015 | Phase 1 |
| NCT03103568 | Swedish Orphan Biovitrum|Parexel |
Drug Drug Interaction
|
March 28, 2017 | Phase 1 |
| NCT03716427 | Cognition Therapeutics |
Healthy Volunteers
|
November 10, 2016 | Phase 1 |
| NCT00185003 | Radboud University Medical Center|ZonMw: The Netherlands Organisation for Health Research and Development |
Endotoxemia
|
January 2003 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 34 mg/mL ( 125.76 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.6989 mL | 18.4945 mL | 36.9891 mL |
| 5 mM | 0.7398 mL | 3.6989 mL | 7.3978 mL |
| 10 mM | 0.3699 mL | 1.8495 mL | 3.6989 mL |
References
- [1] Wray, H.L. and A.W. Harris, Adenosine 3', 5'-monophosphate-dependent protein kinase in adipose tissue: inhibition by tolbutamide. Biochem Biophys Res Commun, 1973. 53(1): p. 291-4.
- [2] Sanchez-Alvarez, R., et al., Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up-regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation. Glia, 2006. 54(2): p. 125-34.
Synonyms
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