2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. DGAT1-IN-3

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.

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

DGAT1-IN-3 Chemical Structure

DGAT1-IN-3 Chemical Structure

CAS No. : 939375-07-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 462 In-stock
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 700 In-stock
50 mg USD 1900 In-stock
100 mg USD 3000 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

DGAT1-IN-3 Related Antibodies

Top Publications Citing Use of Products

View All Acyltransferase Isoform Specific Products:

View All Isoforms
ACAT1 ACAT2 MGAT2 ACAT

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome[1][2].

IC50 & Target

IC50: 38 nM (human DGAT-1); 120 nM (rat DGAT-1)[2]
Cellular Effect
Cell Line Type Value Description References
CHO-K1 EC50
0.66 μM
Compound: 25
Inhibition of human DGAT1 expressed in CHOK1 cells using 14C palmitic acid as substrate after 1 hr by TLC analysis
Inhibition of human DGAT1 expressed in CHOK1 cells using 14C palmitic acid as substrate after 1 hr by TLC analysis
[PMID: 22001092]
CHO-K1 EC50
0.66 μM
Compound: 6
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using [14C]palmitic acid by TLC analysis
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using [14C]palmitic acid by TLC analysis
[PMID: 21413799]
CHO-K1 EC50
0.661 μM
Compound: 6
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]
Sf9 IC50
38 nM
Compound: 5
Inhibition of human DGAT1 expressed in Sf9 cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-Co A substrates incubated for 2 hrs by scintillation counting method
Inhibition of human DGAT1 expressed in Sf9 cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-Co A substrates incubated for 2 hrs by scintillation counting method
[PMID: 23317570]
In Vitro

DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM[1].
DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC50 of 0.66 μM[1].

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

DGAT1-IN-3 Related Antibodies
In Vivo

DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile[2].
DGAT1-IN-3 (50 mg/kg; p.o) exhibits good oral bioavailability (77%) and the maximum exposure level in plasma (Cmax) is 24 μM[2].
DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg)[2].

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

Animal Model: Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)[2]
Dosage: 0, 5, 25, 50 mg/kg; once daily for three weeks
Administration: P.o. administration
Result: Reduced cumulative body weight gain in a dose-dependent manner and was well tolerated in rats.
Animal Model: Male Wistar rats[2]
Dosage: 50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration: P.o. and i.v. administration
Result: Cmax (24 μM); T1/2 (1.95 h).
Molecular Weight

420.39

Formula

C20H19F3N4O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (237.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3787 mL 11.8937 mL 23.7874 mL
5 mM 0.4757 mL 2.3787 mL 4.7575 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

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

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3787 mL 11.8937 mL 23.7874 mL 59.4686 mL
5 mM 0.4757 mL 2.3787 mL 4.7575 mL 11.8937 mL
10 mM 0.2379 mL 1.1894 mL 2.3787 mL 5.9469 mL
15 mM 0.1586 mL 0.7929 mL 1.5858 mL 3.9646 mL
20 mM 0.1189 mL 0.5947 mL 1.1894 mL 2.9734 mL
25 mM 0.0951 mL 0.4757 mL 0.9515 mL 2.3787 mL
30 mM 0.0793 mL 0.3965 mL 0.7929 mL 1.9823 mL
40 mM 0.0595 mL 0.2973 mL 0.5947 mL 1.4867 mL
50 mM 0.0476 mL 0.2379 mL 0.4757 mL 1.1894 mL
60 mM 0.0396 mL 0.1982 mL 0.3965 mL 0.9911 mL
80 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7434 mL
100 mM 0.0238 mL 0.1189 mL 0.2379 mL 0.5947 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

DGAT1-IN-3 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:

DGAT1-IN-3939375-07-2AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT-1obesitydyslipidemiametabolicsyndromeInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
DGAT1-IN-3
Cat. No.:
HY-16434
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.