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T863

Name: T863
Brand: TargetMol
SKU: T4681
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4681Cas No. 701232-20-4

Alias DGAT-3, DGAT-1 inhibitor

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

T863

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Purity: 99.88%

Catalog No. T4681Alias DGAT-3, DGAT-1 inhibitorCas No. 701232-20-4

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$32	In Stock	In Stock
2 mg	$45	In Stock	In Stock
5 mg	$74	In Stock	In Stock
10 mg	$108	In Stock	In Stock
25 mg	$243	In Stock	In Stock
50 mg	$405	In Stock	In Stock
100 mg	$590	In Stock	In Stock
200 mg	$843	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$81	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:99.88%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

T863 AI Summary

T863 inhibits human recombinant DGAT1 with an IC50 of 15.0 nM and rat microsomal DGAT1 with an IC50 of 19.0 nM. It effectively inhibits triacylglycerol synthesis in human HuTu 80 cells with an IC50 of 4.0 nM and in HT-29 cells with an IC50 of 8.0 nM. It shows low inhibitory activity on human DGAT2 and moderate inhibition of human ACAT1 with an IC50 of 12000.0 nM. Pharmacokinetic studies reveal that T863 has high oral bioavailability (>100%) in rats and dogs with moderate to low clearance rates and varying half-lives. In human liver microsomes, it has an apparent clearance of less than 8.0 mL.min-1.kg-1. The compound demonstrates 100% inhibition of plasma triglyceride accumulation at 10 mg/kg in Sprague-Dawley rats and shows significant reductions in plasma triglyceride levels in other animal models. T863 also displays a favorable distribution coefficient (LogD7.4 = 1.32) and good solubility in pH 7.4 buffer. Additionally, it shows potential anti-viral activity by inhibiting SARS-CoV-2 protease activity at 20 µM and demonstrates cell type-dependent effects on cell growth rates and protein stability. However, at high doses, it exhibits toxicity, such as body weight loss in mice and elevated liver enzyme levels in cynomolgus monkeys..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
Synonyms	DGAT-3, DGAT-1 inhibitor

Chemical Properties

Molecular Weight	394.47
Formula	C₂₂H₂₆N₄O₃
Cas No.	701232-20-4
Smiles	CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Relative Density.	1.36 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

DMSO: 41.67 mg/mL (105.64 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (5.07 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	2.5350 mL	12.6752 mL	25.3505 mL	126.7524 mL
5 mM	0.5070 mL	2.5350 mL	5.0701 mL	25.3505 mL
10 mM	0.2535 mL	1.2675 mL	2.5350 mL	12.6752 mL
20 mM	0.1268 mL	0.6338 mL	1.2675 mL	6.3376 mL
50 mM	0.0507 mL	0.2535 mL	0.5070 mL	2.5350 mL
100 mM	0.0254 mL	0.1268 mL	0.2535 mL	1.2675 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