Cat. No.: HY-13749B

Sitagliptin phosphate monohydrate

(Synonyms: MK-0431 phosphate monohydrate)

31 Cited Publications

Customer Review

Based on 31 publication(s) in Google Scholar

Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.

For research use only. We do not sell to patients.

Purity: 99.83%
CAS No.: 654671-77-9
Formula: C₁₆H₂₀F₆N₅O₆P
Molecular Weight:523.32

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Sitagliptin phosphate monohydrate Chemical Structure

CAS No.: 654671-77-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (31)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

DPP-4

19 nM (IC₅₀)

All Dipeptidyl Peptidase Isoforms :

All Endogenous Metabolite Isoforms :

All PKA Isoforms :

All ERK Isoforms :

In Vitro

Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC₅₀ of 19 nM from Caco-2 cell extracts^[1]. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation^[2]. A recent study demonstrates that 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In vivo, the ED₅₀ value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats^[1]. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival^[4]. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 654671-77-9
Appearance Solid
Molecular Weight 523.32
Formula C₁₆H₂₀F₆N₅O₆P
Color White to off-white
SMILES

[H]O[H].O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)C[C@H](N)CC3=CC(F)=C(F)C=C3F.O=P(O)(O)O
Synonyms

MK-0431 phosphate monohydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (31)

All In Vivo Efficacy StudyHistological Imaging/StainingIFRT-PCR

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Journal Impact Factor

J Adv Res

Hippocampal dipeptidyl peptidase 9 bidirectionally regulates memory associated with synaptic plasticity. [Abstract]

2025 Aug:74:225-236. PMID: 39369958
J Nanobiotechnology

Metal-organic-framework-based sitagliptin-release platform for multieffective radiation-induced intestinal injury targeting therapy and intestinal flora protective capabilities. [Abstract]

2024 Oct 16;22(1):631. PMID: 39415273
Gut Microbes

Dual-source DPP4 drives intestinal fibrosis in Crohn's disease: synergistic therapeutic targeting of host and microbiota pathways. [Abstract]

2025 Dec 31;17(1):2593119. PMID: 41334589

Sitagliptin phosphate monohydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119. [Abstract]

Colon length quantification in the DSS group (n = 6) and DSS + DPP4i group (n = 6). Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

Sitagliptin phosphate monohydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119. [Abstract]

Representative H&E-stained colon sections (left) and histologic inflammation scores (right). Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

Sitagliptin phosphate monohydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119. [Abstract]

Representative Masson’s trichrome-stained colon sections and quantification of collagen volume fraction. Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

Sitagliptin phosphate monohydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119. [Abstract]

Immunofluorescence images and quantification of α-SMA⁺ fibrotic thickness in the muscularis propria. Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

Sitagliptin phosphate monohydrate purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119. [Abstract]

RT-qPCR analysis of mRNA levels in colon tissues. Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.
Cell Death Dis

Sitagliptin activates the p62-Keap1-Nrf2 signalling pathway to alleviate oxidative stress and excessive autophagy in severe acute pancreatitis-related acute lung injury. [Abstract]

2021 Oct 11;12(10):928. PMID: 34635643
Int J Biol Macromol

Comprehending the mechanism of catechins against α-glucosidase by multispectral data and their antidiabetic effects in vivo. [Abstract]

2025 Jun 6;318(Pt 1):145051. PMID: 40484085
Biomed Pharmacother

Sitagliptin inhibits the survival, stemness and autophagy of glioma cells, and enhances temozolomide cytotoxicity. [Abstract]

2023 Jun:162:114555. PMID: 36966667
Biochem Pharmacol

Melatonin protects HT-22 cells against palmitic acid-induced glucolipid metabolic dysfunction and cell injuries: Involved in the regulation of synaptic plasticity and circadian rhythms. [Abstract]

2023 Nov:217:115846. PMID: 37804870
J Ethnopharmacol

Eucommia alleviates high fat diet-induced MASLD via the F. prausnitzii/butyrate/GPR43/GLP-1 signaling. [Abstract]

2025 Sep 9;355(Pt A):120587. PMID: 40935212
World J Diabetes

Pig bile powder maintains blood glucose homeostasis by promoting glucagon-like peptide-1 secretion via inhibiting farnesoid X receptor. [Abstract]

2025 Jun 15;16(6):103616. PMID: 40548276
Mol Oncol

Therapeutic strategies for MMAE-resistant bladder cancer through DPP4 inhibition. [Abstract]

2025 Dec 21. PMID: 41422479
Biochim Biophys Acta Mol Basis Dis

Dapagliflozin attenuates AKI to CKD transition in diabetes by activating SIRT3/PGC1-α signaling and alleviating aberrant metabolic reprogramming. [Abstract]

2024 Jul 25:167433. PMID: 39067538
iScience

Non-canonical function of DPP4 promotes cognitive impairment through ERp29-associated mitochondrial calcium overload in diabetes. [Abstract]

2023 Feb 27;26(3):106271. PMID: 36936785
Sci Rep

The In Vitro Biotransformation of the Fusion Protein Tetranectin-Apolipoprotein A1. [Abstract]

2019 Mar 11;9(1):4074. PMID: 30858459
Nutr Neurosci

High-fat diet induces depression-like behaviour in mice associated with changes in microbiome, neuropeptide Y, and brain metabolome. [Abstract]

2019 Dec;22(12):877-893. PMID: 29697017
Exp Cell Res

SOX9 promotes hypoxic pulmonary hypertension through stabilization of DPP4 in pulmonary artery smooth muscle cells. [Abstract]

2024 Sep 12;442(2):114254. PMID: 39276964
Life Metab

Development of cyclopeptide inhibitors specifically disrupting FXR-coactivator interaction in the intestine as a novel therapeutic strategy for MASH. [Abstract]

2025 Feb 8;4(2):loaf004. PMID: 40225300
Front Oncol

Antidiabetic DPP-4 Inhibitors Reprogram Tumor Microenvironment That Facilitates Murine Breast Cancer Metastasis Through Interaction With Cancer Cells via a ROS-NF-кB-NLRP3 Axis. [Abstract]

2021 Sep 24:11:728047. PMID: 34631556
Nutrition

Lactobacillus plantarum NCHBL-004 modulates high-fat diet-induced weight gain and enhances GLP-1 production for blood glucose regulation. [Abstract]

2024 Dec:128:112565. PMID: 39326237
3 Biotech

Neuroprotective effects of DPP-4 inhibitors sitagliptin and vildagliptin in Parkinson's disease via autophagy modulation. [Abstract]

2026 Apr;16(4):146. PMID: 41853215
J Sep Sci

High-throughput bioanalysis of sitagliptin in plasma using direct analysis in real time mass spectrometry and its application in the pharmacokinetic study thereof. [Abstract]

2022 Jan;45(2):631-637. PMID: 34709732
BMC Pharmacol Toxicol

Repurposing DPP-4 inhibitors as anticancer agents in KRAS-mutated pancreatic ductal adenocarcinoma. [Abstract]

2025 Dec 8;26(1):208. PMID: 41361888
Tissue Cell

Saligenin restores insulin responsiveness in lipotoxic myotubes through L-cell-derived GLP-1 via ER stress-autophagy modulation. [Abstract]

2026 Jun 17:103:103704. PMID: 42320358
Korean J Physiol Pharmacol

Sitagliptin attenuates endothelial dysfunction independent of its blood glucose controlling effect. [Abstract]

2021 Sep 1;25(5):425-437. PMID: 34448460
Arch Oral Biol

Sitagliptin regulates the AMPK/NF-κB signaling pathway to alleviate lipopolysaccharide-induced inflammatory responses and promote osteogenic differentiation in rat bone marrow mesenchymal stem cells. [Abstract]

2025 Jul:175:106253. PMID: 40215713
Neurol Res

Sitagliptin rescues memory deficits in Parkinsonian rats via upregulating BDNF to prevent neuron and dendritic spine loss. [Abstract]

2018 Sep;40(9):736-743. PMID: 29781786
bioRxiv

Characterizing the SASP-Dependent Paracrine Spreading of Senescence Between Human Brain Cell Types. [Abstract]

2026 Feb 12:2026.02.10.705129. PMID: 41726875
Orebro University

2024.
Research Square Preprint

2024 Apr 25.
bioRxiv

2023 Nov 4.
Oxid Med Cell Longev

Sitagliptin Alleviates Radiation-Induced Intestinal Injury by Activating NRF2-Antioxidant Axis, Mitigating NLRP3 Inf--lammasome Activation, and Reversing Gut Microbiota Disorder. [Abstract]

2022 May 17;2022:2586305. PMID: 35620578
Oxid Med Cell Longev

DPP4 Inhibitor Attenuates Severe Acute Pancreatitis-Associated Intestinal Inflammation via Nrf2 Signaling. [Abstract]

2019 Nov 15;2019:6181754. PMID: 31827684

Solvent & Solubility

In Vitro:

H₂O : ≥ 33 mg/mL (63.06 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9109 mL

9.5544 mL

19.1088 mL

5 mM

0.3822 mL

1.9109 mL

3.8218 mL

10 mM

0.1911 mL

0.9554 mL

1.9109 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 50 mg/mL (95.54 mM); Clear solution; Need ultrasonic

Protocol

Cell Assay^[2]

CD4T-cells are plated on membrane inserts in serum-free RPMI 1640, and cell migration is assayed using Transwell chambers (Corning), in the presence or absence of purified porcine kidney DPP-4 (32.1 units/mg; 100 mU/mL final concentration) and DPP-4 inhibitor (100 μM). After 1 hour, cells on the upper surface are removed mechanically, and cells that have migrated into the lower compartment are counted. The extent of migration is expressed relative to the control sample.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: Overnight fasted C57BL/6J mice are challenged 45 min after compound administration with an oral glucose load (2 g/kg). Blood samples for glucose measurement are obtained by tail bleed predose and at serial time points after the glucose load. To evaluate the duration of the effect on glucose tolerance, vehicle or DPP-4 inhibitors are administered 16 h before the glucose challenge.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-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 acti [Content Brief]

[2]. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51. [Content Brief]

[3]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a GLP-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73. [Content Brief]

[4]. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9. [Content Brief]

[5]. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	1.9109 mL	9.5544 mL	19.1088 mL	47.7719 mL
	5 mM	0.3822 mL	1.9109 mL	3.8218 mL	9.5544 mL
	10 mM	0.1911 mL	0.9554 mL	1.9109 mL	4.7772 mL
	15 mM	0.1274 mL	0.6370 mL	1.2739 mL	3.1848 mL
	20 mM	0.0955 mL	0.4777 mL	0.9554 mL	2.3886 mL
	25 mM	0.0764 mL	0.3822 mL	0.7644 mL	1.9109 mL
	30 mM	0.0637 mL	0.3185 mL	0.6370 mL	1.5924 mL
	40 mM	0.0478 mL	0.2389 mL	0.4777 mL	1.1943 mL
	50 mM	0.0382 mL	0.1911 mL	0.3822 mL	0.9554 mL
	60 mM	0.0318 mL	0.1592 mL	0.3185 mL	0.7962 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Sitagliptin phosphate monohydrate

31 Cited Publications

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Sitagliptin phosphate monohydrate

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Publications Citing Use of MedChemExpress (MCE) Sitagliptin phosphate monohydrate

All Dipeptidyl Peptidase Isoforms

All Endogenous Metabolite Isoforms

All PKA Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Publications (31)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Sitagliptin phosphate monohydrate Related Classifications

HY-13749B Related Classifications