Catalog No.S5079 Synonyms: MK-0431

For research use only.

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 Chemical Structure

CAS No. 486460-32-6

Selleck's Sitagliptin has been cited by 14 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.
DPP-4 [1]
18 nM
In vitro

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)[1]. MK0431 reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. 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[3].

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[1]. 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[4]. 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[5]. 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[6].

Protocol (from reference)

Cell Research:


  • Cell lines: CD4+ T-cells
  • Concentrations: 100 μmol/l
  • Incubation Time: 1 h
  • Method:

    CD4+ T-cells (1 × 106 cells) were plated on membrane inserts (8-μm pore size) in serum-free RPMI 1640 medium. Cell migration was assayed using Transwell chambers in media ± purified porcine kidney DPP-IV (32.1 units/mg; 100 mU/ml final concentration) ± sitagliptin (100 μmol/l) or human GIP (100 nmol/l) or human GLP-1 (100 nmol/l). After 1 h, cells on the upper surface were removed mechanically and migrated cells in the lower compartment were counted.

Animal Research:


  • Animal Models: male ICR mice
  • Dosages: 280 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 407.31


CAS No. 486460-32-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)CC(CC3=CC(=C(C=C3F)F)F)N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05219409 Not yet recruiting Drug: Sitagliptin|Device: Professional CGM Type 1 Diabetes University of Milan December 2022 Phase 2|Phase 3
NCT05403281 Completed Drug: DW6012 Healthy Subjects Dong Wha Pharmaceutical Co. Ltd. November 5 2021 Phase 1
NCT03359590 Completed Drug: Sitagliptin 100 mg|Drug: Placebo Pharmacological Action Profil Institut für Stoffwechselforschung GmbH|Merck Sharp & Dohme LLC March 21 2018 Phase 2
NCT03659461 Completed Drug: Sitagliptin Type 2 Diabetes Mellitus|PreDiabetes National University of Malaysia October 1 2017 Not Applicable
NCT03233178 Completed Other: Non-interventional T2DM (Type 2 Diabetes Mellitus)|Fatty Liver|NAFLD LMC Diabetes & Endocrinology Ltd. January 2017 --

(data from, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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