2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. AZD3988

AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity.

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AZD3988 Chemical Structure

AZD3988 Chemical Structure

CAS No. : 892489-52-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

AZD3988 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

AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity[1].

IC50 & Target

IC50: 0.6 nM (h DGAT-1), 0.5 nM (Rat DGAT-1), 1.1 nM (Mouse DGAT-1)[1]
Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
0.0006 μM
Compound: 53, AZD3988
Inhibition of human recombinant DGAT1 expressed in baculovirus infected insect sf9 cells using [14C] oleoyl coenzyme A after 30 mins by scintillation counting
Inhibition of human recombinant DGAT1 expressed in baculovirus infected insect sf9 cells using [14C] oleoyl coenzyme A after 30 mins by scintillation counting
[PMID: 22608962]
Sf9 IC50
36 nM
Compound: 6
Inhibition of human DGAT1 expressed in Sf9 insect cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-CoA substrate by scintillation counting analysis
Inhibition of human DGAT1 expressed in Sf9 insect cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-CoA substrate by scintillation counting analysis
[PMID: 24900877]
In Vitro

AZD3988 (compound 53) (10 μM) can inhibit DGAT-1 with IC50 values of 0. 6 nM (human), 0. 5nM (rat), 1.1 nM (mouse) and 0.5 nM (HuTu 80 cell), respectively[1].

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

AZD3988 Related Antibodies
In Vivo

AZD3988 (compound 53) shows (i.v., p.o.; 0.5, 1, 2, 5 mg/kg) has good pharmacokinetics in vivo efficacy[1].

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

Animal Model: Mouse, Rats and Dog[1]
Dosage: 0.5, 1, 2, 5 mg/kg
Administration: IV at 0.5 mg/kg (mouse), 2 mg/kg (rat) and 1 mg/kg (dog) and po at 1 mg/kg (mouse), 5 mg/kg(rat) and 1 mg/kg (dog)
Result:
Species Clp (mL/min/kg) Vdss(L/kg) IV half-life (h) po half-life (h) po Cmax(lM) Bioavailability (%)
Mouse 4.6 0.99 4.9 4.7 1.9 >100
Rat 1.1 0.35 3.4 5.8 20 >100
Dog 2.5 0.36 1.8 5.7 1.5 32
Molecular Weight

456.44

Formula

C23H22F2N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C=C1)[C@H](CC2)CC[C@@H]2CC(O)=O)C3=NN=C(NC4=CC=C(C(F)=C4)F)O3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (36.52 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 2.1909 mL 10.9543 mL 21.9087 mL
5 mM 0.4382 mL 2.1909 mL 4.3817 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. 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
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (3.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.67 mg/mL (3.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 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 (16.7 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 (251 KB)

COA (245 KB) HNMR (141 KB) RP-HPLC (170 KB) LCMS (384 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, 6 months; -20°C, 1 month. 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 2.1909 mL 10.9543 mL 21.9087 mL 54.7717 mL
5 mM 0.4382 mL 2.1909 mL 4.3817 mL 10.9543 mL
10 mM 0.2191 mL 1.0954 mL 2.1909 mL 5.4772 mL
15 mM 0.1461 mL 0.7303 mL 1.4606 mL 3.6514 mL
20 mM 0.1095 mL 0.5477 mL 1.0954 mL 2.7386 mL
25 mM 0.0876 mL 0.4382 mL 0.8763 mL 2.1909 mL
30 mM 0.0730 mL 0.3651 mL 0.7303 mL 1.8257 mL
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AZD3988 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:

AZD3988892489-52-0AZD 3988AZD-3988AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseoraldiacylglycerol acyl transferase-1 (DGAT-1)High throughput screening (HTS)metabolic diseasesdiabetesobesityInhibitorinhibitorinhibit

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