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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
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Snowprint: a predictive tool for genetic biosensor discovery
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), steroid (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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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
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:
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 << |
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 |
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Dissolving Methods |
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. 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:
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