Sitagliptin

Catalog No.S5079 Synonyms: MK-0431

Molecular Weight(MW): 407.31

Sitagliptin 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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Cited by 2 publications

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Description

Sitagliptin 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]	+ Expand 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]	+ Expand Animal Models: male ICR mice Formulation: pre-mixed with high fat diet Dosages: 280 mg/kg Administration: oral (Only for Reference)

Cell Research:

^[5]

+ Expand

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]

+ Expand

Animal Models: male ICR mice
Formulation: pre-mixed with high fat diet
Dosages: 280 mg/kg
Administration: oral
(Only for Reference)

References

+ Expand

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
Storage	2 years -80°C in solvent
Synonyms	MK-0431

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03790839	Not yet recruiting	Patients	Hua Medicine Limited	January 2019	Phase 1
NCT03790839	Not yet recruiting	Patients	Hua Medicine Limited	January 2019	Phase 1
NCT03738878	Recruiting	Hypertension	Vanderbilt University Medical Center	November 15 2018	Phase 4
NCT03738878	Recruiting	Hypertension	Vanderbilt University Medical Center	November 15 2018	Phase 4
NCT03602638	Not yet recruiting	Atherosclerosis Type 2 Diabetes Mellitus Dipeptidyl Peptidase-4 Inhibitor GLP-1	Chinese PLA General Hospital	October 1 2018	Phase 4
NCT03602638	Not yet recruiting	Atherosclerosis Type 2 Diabetes Mellitus Dipeptidyl Peptidase-4 Inhibitor GLP-1	Chinese PLA General Hospital	October 1 2018	Phase 4

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