Art. -Nr.: HY-50861

AZD3988

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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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Reinheit: 99.89%
CAS. Nr.: 892489-52-0
Formel: C₂₃H₂₂F₂N₄O₄
Molecular Weight:456.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZD3988 Chemical Structure

CAS. Nr.: 892489-52-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.6 nM (h DGAT-1), 0.5 nM (Rat DGAT-1), 1.1 nM (Mouse DGAT-1)^[1]

Alle Acyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HuTu80	IC₅₀	0.0005 μM Compound: 53, AZD3988	Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells	[PMID: 22608962]
HuTu80	IC₅₀	0.5 nM Compound: 53, AZD3988	Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells	[PMID: 22608962]
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	0.6 nM 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.

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)	V_dss(L/kg)	IV half-life (h)	po half-life (h)	po C_max(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

Chemical Information

CAS. Nr. 892489-52-0
Appearance Solid
Molecular Weight 456.44
Formel C₂₃H₂₂F₂N₄O₄
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1909 mL

10.9543 mL

21.9087 mL

5 mM

0.4382 mL

2.1909 mL

4.3817 mL

10 mM

0.2191 mL

1.0954 mL

2.1909 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. McCoull W, et al. Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AZD3988

1 Cited Publications

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AZD3988

Metabolism/Protease Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AZD3988

Alle Acyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZD3988

Metabolism/Protease Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AZD3988

Alle Acyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZD3988 Related Classifications

HY-50861 Related Classifications