Sitagliptin

Name: Sitagliptin
Brand: Selleck Chemicals
SKU: S5079
Rating: 5 (11 reviews)

For research use only.

Catalog No.S5079 Synonyms: MK-0431

11 publications

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.

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Selleck's Sitagliptin has been cited by 11 publications

Med Sci Monit, 2021, 27:e928933

PubMed: 33735157 ( click the link to review the publication )

J Biol Chem, 2020, 10.1074/jbc.RA119.010894

PubMed: 31988243 ( click the link to review the publication )

J Diabetes Res, 2020, 2020:2450781

PubMed: 32566677 ( click the link to review the publication )

Arthritis Rheumatol, 2019, 101002/art41058

PubMed: 31350829 ( click the link to review the publication )

Cancer Res, 2018, 78(22):6354-6362

PubMed: 30242112 ( click the link to review the publication )

Am J Physiol Lung Cell Mol Physiol, 2018, 315(5):L834-L845

PubMed: 30188745 ( click the link to review the publication )

J Cardiovasc Pharmacol Ther, 2018, 23(1):66-78

PubMed: 28618859 ( click the link to review the publication )

Cardiovasc Drugs Ther, 2018, 32(6):541-552

PubMed: 30328028 ( click the link to review the publication )

Exp Hematol, 2018, 57:50-59.e6

PubMed: 29031704 ( click the link to review the publication )

Islets, 2018, 10(5):175-180

PubMed: 30142012 ( click the link to review the publication )

FEMS Microbiol Lett, 2016, 363(9)

PubMed: 27010012 ( click the link to review the publication )

Purity & Quality Control

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Biological Activity

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.

Targets

DPP-4 ^[1]
(Cell-free)

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

Cell Research:

^[5]

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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.

(Only for Reference)

Animal Research:

^[4]

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Animal Models: male ICR mice
Dosages: 280 mg/kg
Administration: oral
(Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	81 mg/mL (198.86 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	407.31
Formula	C₁₆H₁₅F₆N₅O
CAS No.	486460-32-6
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	MK-0431
Smiles	C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)CC(CC3=CC(=C(C=C3F)F)F)N

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

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

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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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DPP-4 Signaling Pathway Map

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Sitagliptin