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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
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]

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Batch Information

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Purity:99.91%

Resource Download

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
Color	White
Appearance	Solid

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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