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Trelagliptin

Name: Trelagliptin
Brand: TargetMol
SKU: T6237
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6237Cas No. 865759-25-7

Alias SYR-472

Trelagliptin (SYR-472) is a highly specific, long-acting DPP-4 inhibitor.

Trelagliptin

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Purity: 98.88%

Catalog No. T6237Alias SYR-472Cas No. 865759-25-7

Trelagliptin (SYR-472) is a highly specific, long-acting DPP-4 inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$41	In Stock	In Stock
10 mg	$66	In Stock	In Stock
25 mg	$85	In Stock	In Stock
50 mg	$101	In Stock	In Stock
100 mg	$134	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$45	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:98.88%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Trelagliptin AI Summary

Trelagliptin exhibits potent inhibitory activity against human DPP4, with reported IC50 values ranging from 1.3 nM to 4.0 nM, and shows a stabilizing effect on the enzyme-substrate complex with a dissociation half-life of 0.5 hours. It has high metabolic stability and a prolonged half-life in both rat and human liver microsomes, indicating durable action and slow clearance. The compound impacts several cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4, with IC50 values below 10,000 nM, which may affect drug metabolism. Despite its promising pharmacokinetic profile and good oral bioavailability, Trelagliptin exhibits limited antiviral activity against SARS-CoV-2 and modest inhibitory activity against the human HDAC6 enzyme. Nonetheless, its significant anti-diabetic activity, as evidenced by lowered blood glucose and increased insulin secretion in mice models, highlights its potential as a therapeutic agent for diabetes..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Trelagliptin (SYR-472) is a highly specific, long-acting DPP-4 inhibitor.
Targets&IC50	DPP4:4 nM (IC50)
Synonyms	SYR-472

Chemical Properties

Molecular Weight	357.38
Formula	C₁₈H₂₀FN₅O₂
Cas No.	865759-25-7
Smiles	Cn1c(=O)cc(N2CCC[C@@H](N)C2)n(Cc2cc(F)ccc2C#N)c1=O
Relative Density.	1.38 g/cm3 (Predicted)

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

Ethanol: 3 mg/mL (8.39 mM), Heating is recommended.

DMSO: 55 mg/mL (153.9 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.6 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7981 mL	13.9907 mL	27.9814 mL	139.9071 mL
5 mM	0.5596 mL	2.7981 mL	5.5963 mL	27.9814 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2798 mL	1.3991 mL	2.7981 mL	13.9907 mL
20 mM	0.1399 mL	0.6995 mL	1.3991 mL	6.9954 mL
50 mM	0.0560 mL	0.2798 mL	0.5596 mL	2.7981 mL
100 mM	0.0280 mL	0.1399 mL	0.2798 mL	1.3991 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