2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. T863

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.

CAS No. : 701232-20-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 14 publication(s) in Google Scholar

T863 Related Antibodies

Top Publications Citing Use of Products

    T863 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Aug 13;121(33):e2406492121.

    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.

    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.

    View All Acyltransferase Isoform Specific Products:

    View All Isoforms
    ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2].

    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.

    T863 Related Antibodies
    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.
    Appearance

    Solid

    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
    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
    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)

    Mass
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    Concentration
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    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)

    g

    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: 99.83%

    SDS (393 KB)

    COA (247 KB) LCMS (89 KB)

    Handling Instructions (2659 KB)
    References

    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
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    T863 Related Classifications

    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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