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Sitagliptin phosphate

Name: Sitagliptin phosphate
Brand: TargetMol
SKU: T23358
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T23358Cas No. 654671-78-0

Alias Sitagliptin (phosphate), MK-0431 phosphate, Januvia

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Sitagliptin phosphate

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Purity: 99.91%

Catalog No. T23358Alias Sitagliptin (phosphate), MK-0431 phosphate, JanuviaCas No. 654671-78-0

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$33	In Stock	In Stock
100 mg	$47	In Stock	In Stock
200 mg	$57	In Stock	In Stock
500 mg	$94	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$52	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.91%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.
Targets&IC50	DPP4:19 nM
In vitro	In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM. Sitagliptin inhibited DPP-8 (IC50: 48 μM). Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and aminopeptidase P [1].
In vivo	In free-fed Han-Wistar rats, the ED50 values ??for the inhibition of plasma DPP-4 activity by sitagliptin phosphate were calculated as 7 hours post-dose at 2.3 mg/kg and 24 hours post-dose at 30 mg/kg [1]. A mouse model of streptozotocin-induced type 1 diabetes showed elevated plasma DPP-4 levels, which was significantly suppressed in mice on a sitagliptin phosphate diet. This is achieved through a positive effect on hyperglycemia regulation, possibly by prolonging islet graft survival. The plasma clearance and volume of distribution of sitagliptin phosphate in rats (40-48 mL/min/kg, 7-9 L/kg) were higher than those in dogs (9 mL/min/kg, 3 L/kg); its The half-life is shorter in rats, 2 hours in dogs and 4 hours in dogs[2].
Synonyms	Sitagliptin (phosphate), MK-0431 phosphate, Januvia

Chemical Properties

Molecular Weight	505.31
Formula	C₁₆H₁₈F₆N₅O₅P
Cas No.	654671-78-0
Smiles	N[C@@H](CC(N1Cc2nnc(C(F)(F)F)n2CC1)=O)Cc(c(F)c1)cc(F)c1F.OP(O)(O)=O
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (98.95 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9790 mL	9.8949 mL	19.7898 mL	98.9492 mL
5 mM	0.3958 mL	1.9790 mL	3.9580 mL	19.7898 mL
10 mM	0.1979 mL	0.9895 mL	1.9790 mL	9.8949 mL
20 mM	0.0989 mL	0.4947 mL	0.9895 mL	4.9475 mL
50 mM	0.0396 mL	0.1979 mL	0.3958 mL	1.9790 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc