T863

Name: T863
Brand: MedChemExpress
SKU: HY-32219
Rating: 5.0 (9 reviews)

Cat. No.: HY-32219 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1) inhibitor with an IC₅₀ of 15 nM. T863 has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.

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

T863 Chemical Structure

CAS No. : 701232-20-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 101	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 101	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 139	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 301	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 502	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 884	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE T863

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View All Isoforms

ACAT1 ACAT2 MGAT2 ACAT

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 15 nM (DGAT1)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	1.436 μM Compound: 3	Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay	[PMID: 21413799]
HT-29	IC₅₀	16 nM Compound: 1	Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting	[PMID: 24900321]
HT-29	IC₅₀	8 nM Compound: 2	Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay	[PMID: 21908190]
HuTu80	IC₅₀	0.004 μM Compound: 2	Inhibition of triacylglycerol synthesis in human HuTu 80 cells after 30 mins Inhibition of triacylglycerol synthesis in human HuTu 80 cells after 30 mins	[PMID: 19256504]
Sf9	IC₅₀	0.015 μM Compound: 2	Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography	[PMID: 19256504]
Sf9	IC₅₀	72 nM Compound: 1	Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation counting Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation counting	[PMID: 24900321]

In Vitro

T863 (for 3 days) enhanceS insulin-stimulated glucose uptake, suggesting a possible role for adipocytes to improve insulin sensitivity upon DGAT1 inhibition in differentiated 3T3-L1 adipocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

T863 (30 mg/kg; oral administration) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL6 normal mice (8 weeks old) or diet-induced obese (DIO) mice (10 months old, fed a high fat diet for 8 months)^[1]
Dosage:	30 mg/kg (5 μL/g)
Administration:	Oral administration; once a day for days 1-7 and twice a day for days 8-14
Result:	Significantly delayed fat absorption and resulted in lipid accumulation in the distal small intestine of mice, mimicking the effects of genetic ablation of DGAT1.

Molecular Weight

394.47

Formula

C₂₂H₂₆N₄O₃

CAS No.

701232-20-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C[C@H]1CC[C@H](C2=CC=C(C3=NC4=C(N)N=CN=C4OC3(C)C)C=C2)CC1

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 : ≥ 50 mg/mL (126.75 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	2.5350 mL	12.6752 mL	25.3505 mL
5 mM	0.5070 mL	2.5350 mL	5.0701 mL
10 mM	0.2535 mL	1.2675 mL	2.5350 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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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.

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: 99.97%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (247 KB) HNMR (209 KB) RP-HPLC (195 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Cao J, et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases. J Biol Chem. 2011 Dec 2;286(48):41838-51. [Content Brief]

[2]. Alan M Birch, et al. Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. J Med Chem. 2009 Mar 26;52(6):1558-68. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5350 mL	12.6752 mL	25.3505 mL	63.3762 mL
	5 mM	0.5070 mL	2.5350 mL	5.0701 mL	12.6752 mL
	10 mM	0.2535 mL	1.2675 mL	2.5350 mL	6.3376 mL
	15 mM	0.1690 mL	0.8450 mL	1.6900 mL	4.2251 mL
	20 mM	0.1268 mL	0.6338 mL	1.2675 mL	3.1688 mL
	25 mM	0.1014 mL	0.5070 mL	1.0140 mL	2.5350 mL
	30 mM	0.0845 mL	0.4225 mL	0.8450 mL	2.1125 mL
	40 mM	0.0634 mL	0.3169 mL	0.6338 mL	1.5844 mL
	50 mM	0.0507 mL	0.2535 mL	0.5070 mL	1.2675 mL
	60 mM	0.0423 mL	0.2113 mL	0.4225 mL	1.0563 mL
	80 mM	0.0317 mL	0.1584 mL	0.3169 mL	0.7922 mL
	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6338 mL

T863 Related Classifications

Metabolic Disease

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:

T863701232-20-4T 863T-863AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT1orally activetriacylglycerolInhibitorinhibitorinhibit

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T863

Customer Review

T863 Related Antibodies

9 Publications Citing Use of MCE T863

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Acyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

T863 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

T863 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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