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Chemical Structure| 486460-32-6 Chemical Structure| 486460-32-6
Chemical Structure| 486460-32-6

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CAS No.: 486460-32-6

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Sitagliptin is a DPP-4 inhibitor with high affinity for the DPP-4 enzyme, with an IC50 value of 19 nM. Sitagliptin has hypoglycemic effects and can be used in research on type 2 diabetes.

Synonyms: MK-0431

4.5 *For Research Use Only !

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Product Citations

Product Citations

Simon d’Oelsnitz ; Sarah K. Stofel ; Joshua D. Love ; Andrew D. Ellington ;

Abstract: Bioengineers increasingly rely on ligand-inducible transcription regulators for chemical-responsive control of gene expression, yet the number of regulators available is limited. Novel regulators can be mined from genomes, but an inadequate understanding of their DNA specificity complicates genetic design. Here we present Snowprint, a simple yet powerful bioinformatic tool for predicting regulator:operator interactions. Benchmarking results demonstrate that Snowprint predictions are significantly similar for >45% of experimentally validated regulator:operator pairs from organisms across nine phyla and for regulators that span five distinct structural families. We then use Snowprint to design promoters for 33 previously uncharacterized regulators sourced from diverse phylogenies, of which 28 are shown to influence gene expression and 24 produce a >20-fold dynamic range. A panel of the newly repurposed regulators are then screened for response to biomanufacturing-relevant compounds, yielding new sensors for a polyketide (olivetolic acid), terpene (geraniol), (ursodiol), and alkaloid (tetrahydropapaverine) with induction ratios up to 10.7-fold. Snowprint represents a unique, protein-agnostic tool that greatly facilitates the discovery of ligand-inducible transcriptional regulators for bioengineering applications.

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Product Details of Sitagliptin

CAS No. :486460-32-6
Formula : C16H15F6N5O
M.W : 407.31
SMILES Code : O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)C[C@H](N)CC3=CC(F)=C(F)C=C3F
Synonyms :
MK-0431
MDL No. :MFCD19684081
InChI Key :MFFMDFFZMYYVKS-SECBINFHSA-N
Pubchem ID :4369359

Safety of Sitagliptin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Rat VM neuronal cultures 100 μM 6-OHDA 2 hours To evaluate the protective effects of GLP-1 and GIP against 6-OHDA-induced neuronal damage, results showed that the combination of GLP-1 and GIP significantly mitigated 6-OHDA-induced neuronal damage. PMC11336009
Bone marrow-derived dendritic cells (BMDCs) 0.3 mM and 0.5 mM 24 hours To investigate the effect of Sitagliptin on gene expression in BMDCs, the results showed that the expression patterns of various genes in BMDCs treated with sitagliptin closely resembled those observed in cDC1s following the uptake of tumor antigens. PMC10921530
DC2.4 cells 100 ng/mL 24 hours To investigate the effect of CXCL10 on the activation of DC2.4 cells, the results showed that CXCL10 treatment significantly increased the expression of DC activation markers CD40 and CD80. PMC10921530
Rat mesangial cells 0.1, 1, 10 μmol/ml 24 hours To investigate the protective effect of Sitagliptin on high glucose-induced rat mesangial cells and its possible mechanism, the results showed that Sitagliptin inhibited renal fibrosis by regulating the TGF-β1/Smad pathway. PMC5846674
SKOV-3 cells 50 μM 24 hours Sitagliptin induced caspase 3/7 activation in paclitaxel-treated SKOV-3 cells, reduced migration and invasiveness of SKOV-3 cells, and decreased concentrations of MMP-1, MMP-2, MMP-7, MMP-10, TIMP-1, TIMP-2. PMC7731375
OVCAR-3 cells 50 μM 24 hours Sitagliptin induced caspase 3/7 activation in paclitaxel-treated OVCAR-3 cells. PMC7731375
Endothelial Progenitor Cells (EPCs) 3 μM 24 hours Sitagliptin pretreatment significantly prevented high glucose-induced EPC apoptosis and tube formation impairment, and reduced oxidative stress. PMC5742710
MoDCs 500 μg/mL 4 days To investigate the effect of Sitagliptin on the differentiation and functions of MoDCs. Sitagliptin impaired differentiation and maturation of MoDCs, reduced the expression of CD40, CD83, CD86, NLRP3, and HLA-DR, increased the expression of CD26, ILT4, and IDO1, and inhibited the production of IL-1β, IL-12p70, IL-23, and IL-27, while increasing the production of IL-10 and TGF-β. PMC10706581
DLD-1 cells 140 μM 48 hours Evaluate the effect of Sitagliptin on the viability of DLD-1 cells, results showed that Sitagliptin significantly reduced the viability of DLD-1 cells PMC10778938
HCT116 cells 270 μM 48 hours Evaluate the effect of Sitagliptin on the viability of HCT116 cells, results showed that Sitagliptin significantly reduced the viability of HCT116 cells PMC10778938
SH-SY5Y cells 10 and 100 nM 48 hours To evaluate the neuroprotective and neurotrophic effects of GLP-1 and GIP, results showed that the combination of GLP-1 and GIP had significant neuroprotective and neurotrophic effects in neuronal cultures. PMC11336009
H9c2 cardiomyocytes 50, 100 nM 6 hours Sitagliptin significantly alleviated H/R-induced damages in H9c2 cardiomyocytes, mitigated oxidative stress and mitochondrial dysfunction, and suppressed excessive autophagy and mitophagy. PMC9276022

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
C57BL/6 or BALB/c mice MC38-EGFP and MC38-OVA tumor models Oral 0.011 Daily administration until the end of the experiment To investigate the inhibitory effect of Sitagliptin on tumor growth, the results showed that Sitagliptin significantly inhibited tumor growth and enhanced cDC1-mediated antigen presentation and T cell activation. PMC10921530
Rats Trpv2+/? rat model Topical eye drops 10 mg/mL Twice daily for two weeks To evaluate the protective effect of Sitagliptin eye drops on the retinal neurovascular unit in Trpv2+/? rats, the results showed that Sitagliptin significantly prevented retinal thinning, vasodilation, inflammation, oxidative stress, and glial activation. PMC11607821
Rats Type 2 diabetic nephropathy model Oral 10 mg/kg Once daily for 12 weeks To evaluate the therapeutic effect of Sitagliptin on type 2 diabetic nephropathy rats, the results showed that Sitagliptin significantly alleviated renal injury and fibrosis by inhibiting the TGF-β1/Smad pathway. PMC5846674
Wistar albino rats Streptozotocin-induced type 2 diabetes model Oral 100 mg/kg Once daily for four weeks Sitagliptin mitigated diabetic nephropathy, reduced inflammatory biomarkers, and improved kidney structure. PMC10095069
Rats 6-OHDA unilateral lesion model Oral 10 mg/kg and 30 mg/kg Once daily for 35 or 45 days To evaluate the neuroprotective and neuroregenerative effects of Sitagliptin in the 6-OHDA-induced Parkinson's disease model, results showed that Sitagliptin significantly mitigated 6-OHDA-induced dopaminergic neurodegeneration and rotational behavior, and enhanced neurogenesis. PMC11336009
db/db mice Diabetic hind limb ischaemia model Oral 25 mg/kg Once daily for 1 week or 35 days Sitagliptin treatment significantly enhanced ischaemic angiogenesis and blood perfusion in diabetic mice, and increased circulating EPC numbers. PMC5742710
Wistar rats Diabetic cardiomyopathy model Oral 100 mg/kg/day Once daily for 90 days To investigate the protective effects of sitagliptin against diabetic cardiomyopathy (DCM), focusing on the modulation of the JAK/STAT pathway. Results showed that sitagliptin attenuated DCM by modulating the JAK/STAT signaling pathway. PMC4933570

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00627744 Myocardial Infarction|Unstable... More >> Angina Pectoris|Diabetes Mellitus|Impaired Glucose Tolerance Less << PHASE4 COMPLETED 2025-11-10 Karolinska Institutet, Stockho... More >>lm, 171 76, Sweden|Karolinska University Hospital Solna, Stockholm, Sweden Less <<
NCT01642108 Type 2 Diabetes UNKNOWN 2025-06-13 Nobumasa Ohara, Niigata, 951-8... More >>510, Japan Less <<
NCT02683525 Graft vs Host Disease|Hematopo... More >>ietic Stem Cell Transplantation Less << PHASE2 COMPLETED 2019-10-01 Indiana University Health Hosp... More >>ital, Indianapolis, Indiana, 46202, United States|Indiana University Health Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States Less <<
NCT02406950 Healthy PHASE3 UNKNOWN 2025-08-15 Kyung Hee University Hospital,... More >> Seoul, 130-872, Korea, Republic of Less <<
NCT02650427 Hepato Carcinoma PHASE1 COMPLETED 2025-09-18 Pitié-Salpêtrière Hospital, Pa... More >>ris, 75013, France Less <<
NCT01567540 Hepatitis C PHASE1 TERMINATED 2025-01-14 Centre Hospitalier Victor Dupu... More >>y, Argenteuil, 95100, France|Centre Hospitalier Intercommunal Créteil, Créteil, 94010, France|Henri Mondor Hospital, Créteil, 94010, France|Cochin Hospital, Paris, 75014, France Less <<
NCT01610154 Insulin Secretion|Insulin Resi... More >>stance Less << PHASE4 COMPLETED 2025-06-15 Fuwai Hospital, Beijing, China
NCT03108521 Diabetes Mellitus PHASE4 COMPLETED 2018-10-08 Sichuan provincial people's ho... More >>spital, Chengdu, Sichuan, 610000, China Less <<
NCT02900417 Type 2 Diabetes UNKNOWN 2025-11-16 -
NCT01720264 Acute Myeloid Leukemia|Acute L... More >>ymphoid Leukemia|Hematopoetic Myelodysplasia|Leukemia, Myelogenous, Chronic|Lymphoma, Non-Hodgkin Less << PHASE2 COMPLETED 2017-12-15 Indiana University Melvin and ... More >>Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States|New York Medical College/Westchester Medical Center/Maria Fareri Children's Hosptial, Valhalla, New York, 10595, United States Less <<
NCT04365517 Covid19|Diabetes Mellitus, Typ... More >>e 2|CKD Less << PHASE3 UNKNOWN 2022-12-30 ASST FBF Sacco, Milan, 20157, ... More >>Italy Less <<
NCT00968006 Type 2 Diabetes Mellitus PHASE4 COMPLETED 2025-01-10 University of Padova, Medical ... More >>School, Padova, 35100, Italy Less <<
NCT01721382 Cystic Fibrosis PHASE1 COMPLETED 2025-06-16 Nemours Children's Clinic, Jac... More >>ksonville, Florida, 32207, United States Less <<
NCT02444364 Type 2 Diabetes EARLY_PHASE1 WITHDRAWN 2025-01-16 University of Missouri-Columbi... More >>a: Diabetes Center, Columbia, Missouri, 65212, United States Less <<
NCT03659461 Type 2 Diabetes Mellitus|PreDi... More >>abetes Less << COMPLETED 2020-01-31 Hospital Sultan Ismail, Johor ... More >>Bahru, Johor, 81100, Malaysia Less <<
NCT00686634 Type 2 Diabetes Mellitus PHASE4 COMPLETED 2025-03-10 Charles Drew University of Med... More >>icine and Science, Los Angeles, California, 90059, United States Less <<
NCT05725798 Systemic Inflammatory Response... More >> Syndrome Less << COMPLETED 2023-08-01 University Hospital Münster, M... More >>ünster, North Rhine-Westphalia, 48147, Germany Less <<
NCT01449747 Type 2 Diabetes Mellitus PHASE4 COMPLETED 2025-07-15 The Catholic University of Kor... More >>ea; St.Paul's Hospital, Seoul, 130-709, Korea, Republic of|The Catholic University of Korea; Seoul St. Mary's Hospital, Seoul, 137-701, Korea, Republic of Less <<
NCT00862719 Leukemia, Myeloid, Acute|Acute... More >> Lymphoblastic Leukemia|Myelodysplasia|Leukemia, Myelogenous, Chronic|Lymphoma, Non-Hodgkin Less << PHASE2 COMPLETED 2025-02-15 IU Simon Cancer Center, Indian... More >>apolis, Indiana, 46202, United States Less <<
NCT00967798 Cystic Fibrosis|Prediabetes PHASE3 TERMINATED 2017-12-31 Emory University and Children'... More >>s Healthcare of Atlanta at Egleston, Atlanta, Georgia, 30322, United States|Children's Healthcare of Atlanta at Scottish Rite, Atlanta, Georgia, 30342, United States|Nationwide Children's Hospital, Columbus, Ohio, 43205, United States Less <<
NCT02263677 Type 2 Diabetes|Non-alcoholic ... More >>Fatty Liver Disease Less << PHASE4 WITHDRAWN 2025-01-16 University of Missouri-Columbi... More >>a: Diabetes Center, Columbia, Missouri, 65212, United States Less <<
NCT00960453 Diabetes Mellitus PHASE1 COMPLETED - Clinical Trials Center; Seoul ... More >>National University Hospital, Seoul, 110-744, Korea, Republic of Less <<
NCT00657280 Heart Failure, Congestive EARLY_PHASE1 COMPLETED 2025-02-12 Stanford University School of ... More >>Medicine, Stanford, California, 94305, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.28mL

2.46mL

1.23mL

24.55mL

4.91mL

2.46mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Kim SJ, Nian C, et al. Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes. 2009 Mar;58(3):641-51.

[2]Thomas L, Eckhardt M, et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.

[3]Salles TA, dos Santos L, Barauna VG, Girardi AC. Potential role of dipeptidyl peptidase IV in the pathophysiology of heart failure. Int J Mol Sci. 2015 Feb 16;16(2):4226-49.

[4]R?hrborn D, Wronkowitz N, Eckel J. DPP4 in Diabetes. Front Immunol. 2015 Jul 27;6:386.

[5]Kawasaki T, Chen W, Htwe YM, Tatsumi K, Dudek SM. DPP4 inhibition by sitagliptin attenuates LPS-induced lung injury in mice. Am J Physiol Lung Cell Mol Physiol. 2018 Nov 1;315(5):L834-L845.

[6]Lin CH, Lin CC. Sitagliptin attenuates in?ammatory responses in lipopolysaccharide-stimulated cardiomyocytes via nuclear factor-κB pathway inhibition. Exp Ther Med. 2016 Jun;11(6):2609-2615.

[7]Esposito G, Cappetta D, Russo R, Rivellino A, Ciuffreda LP, Roviezzo F, Piegari E, Berrino L, Rossi F, De Angelis A, Urbanek K. Sitagliptin reduces inflammation, fibrosis and preserves diastolic function in a rat model of heart failure with preserved ejection fraction. Br J Pharmacol. 2017 Nov;174(22):4070-4086.

[8]Davis JA, Singh S, Sethi S, Roy S, Mittra S, Rayasam G, Bansal V, Sattigeri J, Ray A. Nature of action of Sitagliptin, the dipeptidyl peptidase-IV inhibitor in diabetic animals. Indian J Pharmacol. 2010 Aug;42(4):229-33.

 

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