For research use only.
Catalog No.S5079 Synonyms: MK-0431
CAS No. 486460-32-6
Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes.
Selleck's Sitagliptin has been cited by 11 publications
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|Description||Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes.|
Sitagliptin exhibits a > 2600-fold margin of selectivity against DPP8, DPP9, and other members of the dipeptidyl peptidase family (i.e., potency against DPP-4 vs. DPP8/9). MK0431 reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. Sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival.
|In vivo||Sitagliptin is well absorbed after oral administration with a bioavailability of 87%. Sitagliptin has an apparent terminal half-life of 10–12 h at doses of 25-100 mg and is excreted mainly (≈ 80%) as unchanged compound by the kidneys. Sitagliptin does not interfere with the P450 cytochrome enzymes nor have there been any reported significant drug-drug interactions. Sitagliptin has been shown to inhibit DPP-4 activity by > 90% within 1-2 h of administration. It has a short half-life in mice (1-2 h). Chronic sitagliptin treatment in a non-geneticmouse model of type 2 diabetes elicits significant improvement in glycemic control. The improved glucose homeostasis correlates with restoration of normal islet cell (α and β cells) mass, architecture and insulin secretion capacity in response to glucose stimulation. Sitagliptin prolongs islet graft survival in streptozotocin-induced and NOD mice. Administration of sitagliptin in vivo reduces lymph node and splenic CD4+ T-cell migration, measured in vitro, via incretin- and nonincretin-mediated effects, respectively, and splenic sDPP-IV-responsive CD4+ T-cells and lymph node incretin nonresponsive CD4+ T-cells selectively infiltrated islets of diabetic NOD mice, after tail vein injection. Sitagliptin significantly suppressed epileptogenesis in PTZ (pentylenetetrazole)-induced seizures. Sitagliptin counteracted neuronal damage and all biochemical, and histo-chemical alteration induced by PTZ. Oral sitagliptin can promote hippocampal neurogenesis, counteract hippocampal oxidative stress, and prevent the decline in mice cognition.|
-  Karasik A, et al. Curr Med Res Opin. 2008, 24(2):489-96.
-  Kim SJ et al. Diabetes. 2009; 58(3): 641-651.
-  Sangle GV et al. Endocrinology. 2012; 153(2): 564-573.
|In vitro||DMSO||81 mg/mL (198.86 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03359590||Completed||Drug: Sitagliptin 100 mg|Drug: Placebo||Pharmacological Action||Profil Institut für Stoffwechselforschung GmbH|Merck Sharp & Dohme Corp.||March 21 2018||Phase 2|
|NCT03659461||Unknown status||Drug: Sitagliptin||Type 2 Diabetes Mellitus|PreDiabetes||National University of Malaysia||October 1 2017||Not Applicable|
|NCT02900417||Unknown status||Drug: Sitagliptin||Type 2 Diabetes||Second Affiliated Hospital of Soochow University||September 2016||Not Applicable|
|NCT03125694||Completed||Drug: Sitagliptin 100mg|Drug: Pioglitazone 30 mg||Uncontrolled Type 2 Diabetes Mellitus||Tehran University of Medical Sciences||February 1 2015||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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