Cat. No.: HY-10038

A 922500

(Synonyms: DGAT-1 Inhibitor 4a)

31 Cited Publications

Avis client

Based on 31 publication(s) in Google Scholar

A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC₅₀s of 9 and 22 nM against human and mouse DGAT-1, respectively.

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Pureté: 99.33%
CAS No.: 959122-11-3
Formule: C₂₆H₂₄N₂O₄
Masse moléculaire:428.48

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

A 922500 Chemical Structure

CAS No.: 959122-11-3

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (31)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 9 nM (human DGAT-1), 22 nM (mouse DGAT-1)^[1]

Voir tous les produits spécifiques à Isoform Acyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.007 μM Compound: 4a	Inhibition of human recombinant DGAT1 expressed in Sf9 cells Inhibition of human recombinant DGAT1 expressed in Sf9 cells	[PMID: 18183944]
Sf9	IC₅₀	0.024 μM Compound: 4a	Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells	[PMID: 18183944]
Sf9	IC₅₀	20 nM Compound: 4	Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter	[PMID: 21868220]

In Vitro

A 922500 (A-922500) demonstrates excellent selectivity over other acyltransferases, including DGAT-2 (IC₅₀=53 μM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC₅₀=296 μM) ^[1].

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

In Vivo

DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol^[1].

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

Chemical Information

CAS No. 959122-11-3
Appearance Solid
Masse moléculaire 428.48
Formule C₂₆H₂₄N₂O₄
Color Off-white to yellow
SMILES

O=C(NC1=CC=C(C2=CC=C(C([C@@H]3CCC[C@H]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4
Synonyms

DGAT-1 Inhibitor 4a
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (31)

All WBIF

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Journal Impact Factor

Cancer Cell

Multiomic integration reveals tumoral heterogeneity of lipid dependence within lethal group 3 medulloblastoma. [Abstract]

2026 Feb 9;44(2):383-404.e18. PMID: 41544627
Cell Metab

Targeting DGAT1 Ameliorates Glioblastoma by Increasing Fat Catabolism and Oxidative Stress. [Abstract]

2020 Aug 4;32(2):229-242.e8. PMID: 32559414

A 922500 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2020 Aug 4;32(2):229-242.e8. [Abstract]

Effects of Butyrate (But, 1 mM), Valproate (Vpa, 5 mM) and Vorinostat (Vor, 1 μM) on the expression of P-gp and BCRP, NF-кB p65 and phosphorylated p65 (p-p65), and IкBα and phosphorylated IкBα (p-IкBα).

A 922500 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2020 Aug 4;32(2):229-242.e8. [Abstract]

Representative fluorescence imaging and quantification of ROS in U251 cells treated with DGAT1 inhibitor A-922500 (20 mg/mL) for 24 h or shRNA for 48 h in the presence or absence of the CPT1 inhibitor Etomoxir (ETO, 6 mM).
Cell Mol Immunol

Lipid droplets restrict phagosome formation in antifungal immunity. [Abstract]

2025 Apr 7. PMID: 40195475
Mol Cell

An oncogenic JMJD6-DGAT1 axis tunes the epigenetic regulation of lipid droplet formation in clear cell renal cell carcinoma. [Abstract]

2022 Aug 18;82(16):3030-3044.e8. PMID: 35764091
Hepatology

Acetyl-coenzyme A carboxylase alpha promotion of glucose-mediated fatty acid synthesis enhances survival of hepatocellular carcinoma in mice and patients. [Abstract]

2016 Apr;63(4):1272-86. PMID: 26698170
Nat Commun

Lipid droplets sequester palmitic acid to disrupt endothelial ciliation and exacerbate atherosclerosis in male mice. [Abstract]

2024 Sep 27;15(1):8273. PMID: 39333556
Nat Commun

Metabolic reprogramming by Zika virus provokes inflammation in human placenta. [Abstract]

2020 Jun 11;11(1):2967. PMID: 32528049

A 922500 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jun 11;11(1):2967. [Abstract]

The spatiotemporal distribution of LD is analyzed 5 dpi by immunofluorescence. Compared to DMSO control, cells treated with A922500 (DGAT1i) harbor only scarce LDs. Both the number and average volume of LDs are significantly reduced in the presence of DGAT1i.
Adv Sci (Weinh)

Acidosis Forces Fatty Acid Uptake and Metabolism in Cancer Cells Regardless of Genotype. [Abstract]

2025 Jul 29:e05436. PMID: 40726407
Adv Sci (Weinh)

Lipid Droplet-Derived Biomimetic Nanocarriers for the Enhancement of Porcine Intermuscular Fat Content. [Abstract]

2025 May 14:e2406150. PMID: 40365640
Theranostics

GPAT3 is a potential therapeutic target to overcome sorafenib resistance in hepatocellular carcinoma. [Abstract]

2024 Jun 1;14(9):3470-3485. PMID: 38948063
Redox Biol

Chenodeoxycholic acid suppresses AML progression through promoting lipid peroxidation via ROS/p38 MAPK/DGAT1 pathway and inhibiting M2 macrophage polarization. [Abstract]

2022 Oct:56:102452. PMID: 36084349
Int J Biol Sci

Stearoyl-CoA Desaturase-1 dependent lipid droplets accumulation in cancer-associated fibroblasts facilitates the progression of lung cancer. [Abstract]

2022 Oct 18;18(16):6114-6128. PMID: 36439884
J Colloid Interface Sci

Dual metabolic reprogramming by metal-polyphenol nanoplatform enhances ferroptotic therapy for triple-negative breast cancer. [Abstract]

2026 Jul 15:714:140204. PMID: 41780429
Cell Death Dis

Fatty acid synthase-mediated lipid droplet formation enhances macrophage killing of Staphylococcus aureus. [Abstract]

2025 Oct 7;16(1):715. PMID: 41057302
Anal Chem

Live-Cell Multiplexed Imaging and Chemical Sensing with Cumulene and Polyyne Allotropes. [Abstract]

2025 Jul 22;97(28):15393-15401. PMID: 40557718
Front Immunol

Integrated multi-omics reveals the activated retinal microglia with intracellular metabolic reprogramming contributes to inflammation in STZ-induced early diabetic retinopathy. [Abstract]

2022 Sep 2;13:942768. PMID: 36119084
PLoS Pathog

Epstein-Barr virus-transformed B-cells from a hypoxia model of the germinal center requires external unsaturated fatty acids. [Abstract]

2025 Nov 11;21(11):e1013694. PMID: 41218077
Int Immunopharmacol

Targeting lipid peroxidation-associated ferroptosis suppresses lung carcinoma progression by regulating cell cycle arrest. [Abstract]

2024 Jun 24:138:112518. PMID: 38917528
FASEB J

FOXA1 Upregulates HILPDA to Enhance Lipid Droplet Accumulation and Anoikis Resistance in Lung Adenocarcinoma. [Abstract]

2025 Nov 30;39(22):e71249. PMID: 41246996
J Lipid Res

Lipotoxicity of palmitic acid is associated with DGAT1 downregulation and abolished by PPARα activation in liver cells. [Abstract]

2024 Nov 4:100692. PMID: 39505261
J Biol Chem

Neuroinvasive virus facilitates viral replication by employing lipid droplets to reduce arachidonic acid-induced ferroptosis. [Abstract]

2024 Apr;300(4):107168. PMID: 38490434
Sci Rep

Lipidome and metabolome analyses reveal metabolic alterations associated with MCF-7 apoptosis upon 4-hydroxytamoxifen treatment. [Abstract]

2023 Oct 29;13(1):18549. PMID: 37899460
Clin Immunol

The pro-inflammatory effect of triglyceride on human CD4+ T cells and experimental autoimmune uveitis. [Abstract]

2022 Jul:240:109056. PMID: 35659924
J Virol

Lipid Droplets Are Beneficial for Rabies Virus Replication by Facilitating Viral Budding. [Abstract]

2022 Jan 26;96(2):e0147321. PMID: 34757839
Cell Signal

Copper potentiates PUFA-mediated antitumor activity by activating Lipophagy. [Abstract]

2026 Jun:142:112454. PMID: 41765311
Vet Res

Mechanistic role of lipid metabolism in foot-and-mouth disease virus (FMDV) replication. [Abstract]

2026 May 9;57(1):72. PMID: 42106845
Biochim Biophys Acta Mol Cell Biol Lipids

Modulation of lipid droplet biogenesis by p38 MAPK and caspase-1 in docosahexaenoic acid-induced EA.hy926 endothelial cell apoptosis. [Abstract]

2025 Aug 22;1870(8):159683. PMID: 40850528
bioRxiv

2026 Mar 17.
Res Sq

Epstein-Barr Virus-Driven B-Cell Transformation under Germinal Center Hypoxia Requires External Unsaturated Fatty Acids. [Abstract]

2025 Apr 24:rs.3.rs-6506954. PMID: 40313738
bioRxiv

2024 June 12.
bioRxiv

2023 Jul 3.

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (116.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.3338 mL

11.6692 mL

23.3383 mL

5 mM

0.4668 mL

2.3338 mL

4.6677 mL

10 mM

0.2334 mL

1.1669 mL

2.3338 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.83 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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 6.67 mg/mL (15.57 mM); Suspended solution; Need ultrasonic

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

Protocole

Animal Administration^[1]

Mice and Hamsters^[1]
Thirteen-week-old male Golden Syrian hamsters (n=40), initially weighing approximately 140 g, are used. Ten-week-old Male Zucker fatty rats (n=32), weighing between 270 and 330 g, are used. After collection of baseline lipid profiles, hyperlipidemic hamsters (n=10/group) and Zucker fatty rats (n=8/group) are administered vehicle [20:80 (v/v), polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)] or DGAT-1 inhibitor A 922500 (A-922500) at 0.03, 0.3, and 3 mg/kg, once daily by oral gavage. The dosing volume is 5 mL/kg. Serum lipid profiles are then measured 3 h after the dose on day 7 and day 14. Hamsters continue to be fed a high-fat diet with 10% fructose in the drinking water throughout the treatment period. Zucker fatty rats remain on standard rodent diet throughout the study.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (564 KB)
- English - EN (564 KB)
- Français - FR (564 KB)
- Deutsch - DE (564 KB)
- Norwegian - NO (564 KB)
- Español - ES (564 KB)
- Swedish - SV (564 KB)
- Italian - IT (564 KB)
- Korean - KR (564 KB)
- Portuguese - PT (564 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)
Instruction de manipulation (2659 KB)

Références

[1]. King AJ, et al. Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. [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, 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	2.3338 mL	11.6692 mL	23.3383 mL	58.3458 mL
	5 mM	0.4668 mL	2.3338 mL	4.6677 mL	11.6692 mL
	10 mM	0.2334 mL	1.1669 mL	2.3338 mL	5.8346 mL
	15 mM	0.1556 mL	0.7779 mL	1.5559 mL	3.8897 mL
	20 mM	0.1167 mL	0.5835 mL	1.1669 mL	2.9173 mL
	25 mM	0.0934 mL	0.4668 mL	0.9335 mL	2.3338 mL
	30 mM	0.0778 mL	0.3890 mL	0.7779 mL	1.9449 mL
	40 mM	0.0583 mL	0.2917 mL	0.5835 mL	1.4586 mL
	50 mM	0.0467 mL	0.2334 mL	0.4668 mL	1.1669 mL
	60 mM	0.0389 mL	0.1945 mL	0.3890 mL	0.9724 mL
	80 mM	0.0292 mL	0.1459 mL	0.2917 mL	0.7293 mL
	100 mM	0.0233 mL	0.1167 mL	0.2334 mL	0.5835 mL

Keywords

A 922500

31 Cited Publications

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A 922500

Metabolism/Protease Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) A 922500

Voir tous les produits spécifiques à Isoform Acyltransferase

Activité biologique

Chemical Information

Publications (31)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

A 922500

Metabolism/Protease Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) A 922500

Voir tous les produits spécifiques à Isoform Acyltransferase

Activité biologique

Chemical Information

Publications (31)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

A 922500 Related Classifications

HY-10038 Related Classifications