Sitagliptin (Synonyms: MK-0431)

Name: Sitagliptin
Brand: MedChemExpress
SKU: HY-13749
Rating: 5.0 (20 reviews)

Cat. No.: HY-13749 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC₅₀ of 19 nM in Caco-2 cell extracts.

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

Sitagliptin Chemical Structure

CAS No. : 486460-32-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Sitagliptin:

Sitagliptin phosphate monohydrate In-stock
(S)-Sitagliptin phosphate Get quote
(Rac)-Sitagliptin Get quote
(Rac)-Sitagliptin-d4 hydrochloride Get quote
Sitagliptin-d₄ hydrochloride Get quote
Sitagliptin phosphate Get quote

20 Publications Citing Use of MCE Sitagliptin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dipeptidyl Peptidase Isoform Specific Products:

View All Isoforms

DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC₅₀ of 19 nM in Caco-2 cell extracts^[1].

IC₅₀ & Target

DPP-4

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	0.11 μM Compound: sitagliptin, MK-0431	Inhibition of DPP4 in human Caco-2 cells after 60 mins by fluorimetry assay Inhibition of DPP4 in human Caco-2 cells after 60 mins by fluorimetry assay	[PMID: 18243422]
Caco-2	IC₅₀	19 nM Compound: Sitagliptin	Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay	[PMID: 23623674]
Caco-2	IC₅₀	19 nM Compound: sitagliptin	Inhibition of DPP4 extracted from human Caco2 cells using H-Gly-Pro-AMC substrate after 10 mins by fluorescence assay Inhibition of DPP4 extracted from human Caco2 cells using H-Gly-Pro-AMC substrate after 10 mins by fluorescence assay	[PMID: 26005541]
CHO	IC₅₀	147.1 μM Compound: sitagliptin	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	> 100 μM Compound: 4	Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique	[PMID: 22525314]
Sf9	IC₅₀	6.24 nM Compound: 1	Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate	[PMID: 27396490]
Sf9	IC₅₀	6.9 nM Compound: Sitagliptin	Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay	[PMID: 30642693]
U-87MG ATCC	IC₅₀	85.34 μM Compound: Sitagliptin	Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay	[PMID: 32527554]

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].?Stagliptin 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 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.

Clinical Trial

Molecular Weight

407.31

Formula

C₁₆H₁₅F₆N₅O

CAS No.

486460-32-6

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (245.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4551 mL	12.2757 mL	24.5513 mL
5 mM	0.4910 mL	2.4551 mL	4.9103 mL
10 mM	0.2455 mL	1.2276 mL	2.4551 mL

View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (6.14 mM); Clear solution; Need heat to 60°C

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: ≥ 2 mg/mL (4.91 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (279 KB) SDS (557 KB)

COA (247 KB) HNMR (268 KB) LCMS (88 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-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. [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]

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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Thomas, L., 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. [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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4551 mL	12.2757 mL	24.5513 mL	61.3783 mL
	5 mM	0.4910 mL	2.4551 mL	4.9103 mL	12.2757 mL
	10 mM	0.2455 mL	1.2276 mL	2.4551 mL	6.1378 mL
	15 mM	0.1637 mL	0.8184 mL	1.6368 mL	4.0919 mL
	20 mM	0.1228 mL	0.6138 mL	1.2276 mL	3.0689 mL
	25 mM	0.0982 mL	0.4910 mL	0.9821 mL	2.4551 mL
	30 mM	0.0818 mL	0.4092 mL	0.8184 mL	2.0459 mL
	40 mM	0.0614 mL	0.3069 mL	0.6138 mL	1.5345 mL
	50 mM	0.0491 mL	0.2455 mL	0.4910 mL	1.2276 mL
	60 mM	0.0409 mL	0.2046 mL	0.4092 mL	1.0230 mL
	80 mM	0.0307 mL	0.1534 mL	0.3069 mL	0.7672 mL
	100 mM	0.0246 mL	0.1228 mL	0.2455 mL	0.6138 mL

Sitagliptin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sitagliptin486460-32-6MK-0431MK0431MK 0431Dipeptidyl PeptidaseAutophagyDPPInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Sitagliptin (Synonyms: MK-0431)

Customer Review

Other Forms of Sitagliptin:

Sitagliptin Related Antibodies

20 Publications Citing Use of MCE Sitagliptin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dipeptidyl Peptidase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Sitagliptin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Sitagliptin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report