Sitagliptin phosphate monohydrate Potent DPP-4 inhibitor |
Sample solution is provided at 25 µL, 10mM.
2. Ghorpade DS, Ozcan L, et al. "Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance." Nature. 2018 Mar 29;555(7698):673-677. PMID:29562231
3.Mroz PA, Perez-Tilve D, et al. "Native Design of Soluble, Aggregation-Resistant Bioactive Peptides: Chemical Evolution of Human Glucagon." ACS Chem Biol. 2016 Dec 16;11(12):3412-3420. PMID:27797473
4.Khan D, Vasu S, et al. "Islet distribution of Peptide YY and its regulatory role in primary mouse islets and immortalised rodent and human beta-cell function and survival." Mol Cell Endocrinol. 2016 Jul 25;436:102-113. PMID:27465830
5.Gault, V. A., R. Lennox, and P. R. Flatt. "Sitagliptin, a DPP‐4 inhibitor, improves recognition memory, oxidative stress, hippocampal neurogenesis and up‐regulates key genes involved in cognitive decline." Diabetes, Obesity and Metabolism (2015). PMID:25580570
Quality Control & MSDS
- View current batch:
Chemical structure

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Description | Sitagliptin phosphate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. | |||||
Targets | DPP-4 | |||||
IC50 | 19 nM |
Cell experiment [1]: | |
Cell lines |
Endothelial progenitor cells (EPCs) and bone marrow mesenchymalstem cells(MSC) |
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions |
14 d; 25 μmol/L |
Applications |
To determine whether sitagliptin treatment participated in enhancing the differentiation of EPCs and MSCs and cells expressing its ligand, SDF-1α, adipose tissues were co-cultured with sitagliptin (25 μmol/L) in M199 culture medium for 14 d and examined by flow cytometric analysis. The results show that compared with the 7 d cell culture, the numbers of EPCs [CD31/Sca-1+(double-stained) and CXCR4+ (single-stained)] were remarkably higher at day 14 in both the non-sitagliptin-treated (Si-T) group and the Si-T group |
Animal experiment [2]: | |
Animal models |
ApoE−/−mice with the C57BL/6 genetic background |
Dosage form |
200 mg/kg/day; oral taken |
Applications |
In ApoE−/−mice, the sitagliptin group showed fewer atherosclerotic plaques than in controls (7.64±1.98% [range 4.62–10.13%] vs 12.91±1.15% [range 11.55–14.37%], p<0.001). Compared with control mice, atherosclerotic plaque areas decreased respectively 1.92- and 2.74-fold in the aortic root and abdominal aorta of mice fed sitagliptin (p=0.011 and p=0.006). Our data show that sitagliptin can inhibit the formation of atherosclerotic areas in entire aorta, aortic root and abdominal aorta of ApoE−/− mice. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Chua S, Sheu J J, Chen Y L, et al. Sitagliptin therapy enhances the number of circulating angiogenic cells and angiogenesis—evaluations< i> in vitro and in the rat critical limb ischemia model[J]. Cytotherapy, 2013, 15(9): 1148-1163. [2] Zeng Y, Li C, Guan M, et al. The DPP-4 inhibitor sitagliptin attenuates the progress of atherosclerosis in apolipoprotein-E-knockout mice via AMPK-and MAPK-dependent mechanisms[J]. Cardiovascular diabetology, 2014, 13(1): 32. |

Sitagliptin phosphate monohydrate Dilution Calculator

Sitagliptin phosphate monohydrate Molarity Calculator
Cas No. | 654671-77-9 | SDF | Download SDF |
Synonyms | Tesavel, MK-0431,MK0431 | ||
Chemical Name | (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;phosphoric acid;hydrate | ||
Canonical SMILES | [HH].C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)CC(CC3=CC(=C(C=C3F)F)F)N.O.OOP(=O)=O | ||
Formula | C16H15F6N5O.H3PO4.H2O | M.Wt | 523.3 |
Solubility | ≥23.8mg/mL in DMSO | Storage | Store at -20°C |
Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Abstract
The reverse phase UPLC is a method to simultaneously measure Sitagliptin phosphate monohydrate and Metformin hydrochloride in pharmaceutical dosage forms with LOD and LOQ of 0.2 μg/mL and 0.7 μg/mL respectively for Sitagliptin phosphate monohydrate.
Abstract
A retrospective cohort study was performed to investigate the clinical outcomes of sitagliption compared with metformin.
Abstract
The combination of sitagliptin and pioglitazone has been assessed for safety and efficacy in patients with type 2 diabetes.
Abstract
Sitagliptin is a DPP-4 inhibitor that inhibits the cleavage of GLP-1 leading to improved blood glucose control in patients with type 2 diabetes. Although it initially increased the percentage of cells expressing high levels of CD26, sitagliptin failed to alter systemic immune function in healthy volunteers at the end of 28-day treatment.
Abstract
Sitagliptin was evaluated for efficacy and safety in renal transplant recipients.
Sitagliptin phosphate monohydrate is the phosphate salt of its active component, sitagliptin, with one molecule of water. Sitagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4), an enzyme catalyzing the cleavage of peptides with an N-terminal alanine or proline amino acid residue, that selectively inhibits DPP-4 with 50% inhibition concentration IC50 value of 18 nM and shows no affinity towards other DDP enzymes (such as DDP-8 and DDP-9). The inhibition of DPP4 by sitagliptin has been found to be mediated by increasing levels of two DPP-4 substrates, including glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). Sitagliptin is currently being investigated in the treatment of type II diabetes.
Reference
Gallwitz B. Review of sitagliptin phosphate: a novel treatment for type 2 diabetes. Vasc Health Risk Manag. 2007;3(2):203-10.