2. Metabolic Enzyme/Protease
  3. ATP Citrate Lyase
  4. ACLY-IN-3

ACLY-IN-3 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.036 μM and a target Kd of 0.54 μM. ACLY-IN-3 interacts with the allosteric binding site of ACLY to inhibit its activity. ACLY-IN-3 exhibits excellent lipid-lowering effects and alleviates hepatic inflammation and liver fibrosis. ACLY-IN-3 can be used for the research of metabolic dysfunction-associated steatohepatitis.

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

ACLY-IN-3

ACLY-IN-3 Chemical Structure

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ACLY-IN-3 Related Antibodies

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Description

ACLY-IN-3 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.036 μM and a target Kd of 0.54 μM. ACLY-IN-3 interacts with the allosteric binding site of ACLY to inhibit its activity. ACLY-IN-3 exhibits excellent lipid-lowering effects and alleviates hepatic inflammation and liver fibrosis. ACLY-IN-3 can be used for the research of metabolic dysfunction-associated steatohepatitis[1].

In Vitro

ACLY-IN-3 (Compound B1) (50 μM; 4 h) effectively reduces oleic acid-induced lipid accumulation in shNC HepG2 cells via an ACLY-dependent mechanism, with no observed cytotoxicity at concentrations up to 50 μM[1].
ACLY-IN-3 (50 μM; 24 h) suppresses the expression of lipogenic genes FASN, ACC1, and SREBP-1c in oleic acid-induced shNC HepG2 cells via an ACLY-dependent mechanism[1].

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

ACLY-IN-3 Related Antibodies

Real Time qPCR[1]

Cell Line: oleic acid (OA)-induced shNC and shACLY HepG2 cells
Concentration: 50 μM
Incubation Time: 24 h (with 1 mM OA)
Result: In OA-induced shNC HepG2 cells, significantly downregulated mRNA expression of fatty acid synthase (FASN), acetyl-CoA carboxylase 1 (ACC1), and sterol regulatory element-binding protein 1c (SREBP-1c).
Abolished effect in shACLY HepG2 cells.
Parmacokinetics
Species Dose Route Cmax T1/2 AUCinf CL Bioavailability
Mice[1] 10 mg/kg i.p. 1995 ng/mL 8.23 h 2154 ng·h/mL 87 mL/min/kg 124 %
In Vivo

ACLY-IN-3 (Compound B1) (10-30 mg/kg; i.p.; daily; 8 weeks) significantly reduces body weight, hepatic steatosis, systemic insulin resistance, oxidative stress, inflammation, and fibrosis in a high-fat diet-induced murine MASH model[1].

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

Animal Model: C57BL/6J (male, 8 weeks old, 18-20 g, high-fat diet-induced MASH)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; daily; 8 weeks
Result: Reduced average body weight from 49.5 g (HFD group) to 41.7 g (10 mg/kg) and 35.7 g (30 mg/kg).
Significantly lowered elevated serum triglycerides, total cholesterol, alanine aminotransferase, aspartate aminotransferase, and low-density lipoprotein cholesterol, while restoring reduced serum high-density lipoprotein cholesterol to near control levels.
Significantly reduced liver weight, hepatic triglycerides, and hepatic total cholesterol compared to the HFD group.
Achieved near-complete reversal of hepatic lipid accumulation (Oil Red O staining).
Significantly downregulated hepatic mRNA expression of lipogenic markers (FASN, LXR, SREBP-1c, HMGCR, ACC1) and fatty acid uptake marker CD36, while upregulating fatty acid oxidation markers (PPARα, CPT1, PPARγ) and lipid metabolism regulator AMPKα1; confirmed corresponding protein expression changes for FASN, ACC1, and PPARα.
Improved glucose tolerance (reduced OGTT AUC) and insulin sensitivity (reduced ITT AUC) compared to the HFD group.
Significantly reduced hepatic malondialdehyde levels (oxidative stress marker), downregulated mRNA expression of inflammatory markers (CD68, TNF-α, NLRP3, ASC) and pro-fibrotic marker α-SMA, and reduced collagen deposition (Sirius Red staining) in liver tissue.
Restored normal hepatocellular morphology (H&E staining) with no detectable pathological changes in heart, spleen, lung, or kidney tissue.
Molecular Weight

284.26

Formula

C16H12O5
SMILES

O=C1C2=CC(O)=C(C=C2C/C1=C\C3=CC=C(C(O)=C3)O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ACLY-IN-3 Related Classifications

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

ACLY-IN-3ATP Citrate LyaseACLYATP-citrate lyaseinsulin resistanceFASNHepG2 cellsmetabolic dysfunction-associated steatohepatitisSREBP-1coxidative stressACC1hepatic steatosisInhibitorinhibitorinhibit

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