T863
Based on 15 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.83%
- No. CAS: 701232-20-4
- Fòrmula: C22H26N4O3
- Peso molecular:394.47
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Metabolism/Protease Compound Library
HY-L012
-
Orally Active Compound Library
HY-L061
-
Anti-Obesity Compound Library
HY-L087
-
Lipid Metabolism Compound Library
HY-L091
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) T863
More- Nat Metab. 2024 Aug;6(8):1549-1565. [Abstract]
- Cell Mol Immunol. 2025 Apr 7. [Abstract]
- Nat Commun. 2023 May 29;14(1):3100. [Abstract]
- Protein Cell. 2025 Nov 19:pwaf101. [Abstract]
- J Exp Med. 2021 Sep 6;218(9):e20202637. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Aug 13;121(33):e2406492121. [Abstract]
- Mar Life Sci Technol. 2025 Mar 17;7(2):271-283. [Abstract]
- mBio. 2026 Apr 8;17(4):e0336825. [Abstract]
- Aquaculture. 2021 October 15, 543, 736967.
- Biochim Biophys Acta Mol Cell Biol Lipids. 2025 Jun 6:159643. [Abstract]
- Front Oncol. 2021 Apr 22:11:665763. [Abstract]
- Dev Comp Immunol. 2021 Nov:124:104197. [Abstract]
- bioRxiv. 2026 Jun 11:2026.06.10.731372. [Abstract]
- bioRxiv. 2025 May 12.
- bioRxiv. 2024 June 12.
Customer Validation & Images
-
ELISA
-
RT-PCR
-
Cell Imaging/Staining
-
WB
Actividad biológica
IC50: 15 nM (DGAT1)[2]
|
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] |
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.
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.
Chemical Information
-
No. CAS 701232-20-4
-
Appearance Solid
-
Peso molecular 394.47
-
Fòrmula C22H26N4O3
-
Color White to light yellow
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
-
Journal Impact Factor
-
Most Recent
-
Nat Metab
2024 Aug;6(8):1549-1565. PMID: 39143266 -
Cell Mol Immunol
2025 Apr 7. PMID: 40195475 -
Nat Commun
2023 May 29;14(1):3100. PMID: 37248213 -
Protein Cell
Tumor cell-specific loss of GPX4 reprograms triacylglycerol metabolism to escape ferroptosis and impair antitumor immunity in NSCLC. [Abstract]2025 Nov 19:pwaf101. PMID: 41259048 -
J Exp Med
2021 Sep 6;218(9):e20202637. PMID: 34342641
T863 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Sep 6;218(9):e20202637. [Abstract]
IL-1β production and mitochondrial ROS from unstimulated and LPS-ATP–stimulated BMDMs in the presence or absence of T863 (10 μM).
T863 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Sep 6;218(9):e20202637. [Abstract]
Increase in glutathioneized ASCs in T863 (10 μM)-treated BMDM cells.
T863 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Sep 6;218(9):e20202637. [Abstract]
Immunoblot analysis was performed on unstimulated and LPS-ATP-stimulated Ascwt and AscC171A BMDM to detect ASC oligomerization, pro-IL-1β, cleaved IL-1β, pro-caspase-1, and active caspase-1 p20, regardless of T863 (10 μM) treatment, and on both unstimulated and LPS-ATP-stimulated Ascwt BMDM.
-
Proc Natl Acad Sci U S A
Oxysterol binding protein regulates the resolution of TLR-induced cytokine production in macrophages. [Abstract]2024 Aug 13;121(33):e2406492121. PMID: 39361877
T863 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Aug 13;121(33):e2406492121. [Abstract]
BMDMs from WT mice were treated with the indicated Osbp ligand followed by stimulation with LPS or LPS + T863 (50 μM) for 18 h and Il6 measured by ELISA.
-
Mar Life Sci Technol
Emerging role of lipid droplets in obscure puffer immune response against Vibrio harveyi. [Abstract]2025 Mar 17;7(2):271-283. PMID: 40417253 -
mBio
African swine fever virus hijacks lipolysis induced by chaperone-mediated autophagy to upregulate fatty acid β-oxidation and promote viral replication. [Abstract]2026 Apr 8;17(4):e0336825. PMID: 41801037 -
-
Biochim Biophys Acta Mol Cell Biol Lipids
The role of ancient ubiquitous protein 1 (Aup1) in regulating hepatic lipid droplet levels, endoplasmic reticulum stress, and inflammation in zebrafish (Danio rerio). [Abstract]2025 Jun 6:159643. PMID: 40484276 -
Front Oncol
2021 Apr 22:11:665763. PMID: 33968771 -
Dev Comp Immunol
ATF6-DGAT pathway is involved in TLR7-induced innate immune response in Ctenopharyngodon idellus kidney cells. [Abstract]2021 Nov:124:104197. PMID: 34228994 -
bioRxiv
2026 Jun 11:2026.06.10.731372. PMID: 42327215 -
-
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
-
Ficha de datos (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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 |
Powered by Bioz