AZD3988
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.89%
- No. CAS: 892489-52-0
- Fòrmula: C23H22F2N4O4
- Peso molecular:456.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Anti-diabetic Compound Library
HY-L040
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Orally Active Compound Library
HY-L061
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Chemical Probe Library
HY-L063
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Anti-Obesity Compound Library
HY-L087
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Lipid Metabolism Compound Library
HY-L091
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Metabolic Enzyme Compound Library
HY-L146
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Metabolism/Protease Compound Library
HY-L012
Publications Citing Use of MedChemExpress (MCE) AZD3988
More
Actividad biológica
IC50: 0.6 nM (h DGAT-1), 0.5 nM (Rat DGAT-1), 1.1 nM (Mouse DGAT-1)[1]
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Cell Line
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Type | Value | Description | References |
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| HuTu80 | IC50 |
0.0005 μM
Compound: 53, AZD3988
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Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells
Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells
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[PMID: 22608962] |
| HuTu80 | IC50 |
0.5 nM
Compound: 53, AZD3988
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Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells
Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells
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[PMID: 22608962] |
| Sf9 | IC50 |
0.0006 μM
Compound: 53, AZD3988
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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
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[PMID: 22608962] |
| Sf9 | IC50 |
0.6 nM
Compound: 53, AZD3988
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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
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[PMID: 22608962] |
| Sf9 | IC50 |
36 nM
Compound: 6
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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
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[PMID: 24900877] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse, Rats and Dog[1]
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Dosage:0.5, 1, 2, 5 mg/kg
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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)
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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
Chemical Information
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No. CAS 892489-52-0
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Appearance Solid
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Peso molecular 456.44
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Fòrmula C23H22F2N4O4
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
AZD3988 Related Classifications
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