2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. AZD7687

AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research.

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

AZD7687 Chemical Structure

AZD7687 Chemical Structure

CAS No. : 1166827-44-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 250 In-stock
Solution
10 mM * 1 mL in DMSO USD 250 In-stock
Solid
5 mg USD 220 In-stock
10 mg USD 390 In-stock
50 mg USD 1350 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

AZD7687 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AZD7687

View All Acyltransferase Isoform Specific Products:

View All Isoforms
ACAT1 ACAT2 MGAT2 ACAT

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research[1][2].

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
0.43 μM
Compound: 75
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: 23116186]
In Vitro

In an in vitro recombinant mouse, dog, and human DGAT1 enzyme assay, AZD7687 has an IC50 of approximately 100 nM, 60 nM, and 80 nM, respectively. AZD7687 (compound 30) shows inhibition of acyl-CoA:cholesterol acetyltransferase (79% at 10 μM), fatty acid amide hydrolase (IC50 = 3.7 μM), muscarinic M2 receptor (IC50 = 80.5 μM), and phosphodiesterase PDE10A1 (IC50 = 5.5 μM). No activity against human DGAT2 is detected[1][2].

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

AZD7687 Related Antibodies
In Vivo

Prolonged pharmacological inhibition of DGAT1 with AZD7687 in mice results in the same skin phenotype, including sebaceous gland atrophy and alopecia, as seen in the skin of DGAT1-/- mice. AZD7687-mediated effects on the skin were dose- and time-dependent and reversible[3].

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

367.44

Formula

C21H25N3O3
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

CC1=C(C(N)=O)N=C(C2=CC=C([C@H]3CC[C@H](CC(O)=O)CC3)C=C2)C(C)=N1
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 (136.08 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 2.7215 mL 13.6077 mL 27.2153 mL
5 mM 0.5443 mL 2.7215 mL 5.4431 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
=
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 (6.80 mM); Suspended solution; Need ultrasonic and warming

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.80 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
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 2.7215 mL 13.6077 mL 27.2153 mL 68.0383 mL
5 mM 0.5443 mL 2.7215 mL 5.4431 mL 13.6077 mL
10 mM 0.2722 mL 1.3608 mL 2.7215 mL 6.8038 mL
15 mM 0.1814 mL 0.9072 mL 1.8144 mL 4.5359 mL
20 mM 0.1361 mL 0.6804 mL 1.3608 mL 3.4019 mL
25 mM 0.1089 mL 0.5443 mL 1.0886 mL 2.7215 mL
30 mM 0.0907 mL 0.4536 mL 0.9072 mL 2.2679 mL
40 mM 0.0680 mL 0.3402 mL 0.6804 mL 1.7010 mL
50 mM 0.0544 mL 0.2722 mL 0.5443 mL 1.3608 mL
60 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1340 mL
80 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8505 mL
100 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6804 mL
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AZD7687 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:

AZD76871166827-44-6AZD 7687AZD-7687AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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