2. Others Metabolic Enzyme/Protease NF-κB Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor
  3. Drug Derivative Acyltransferase NF-κB PPAR Fatty Acid Synthase (FASN) Keap1-Nrf2
  4. Esculeogenin A

Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.

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

Esculeogenin A

Esculeogenin A Chemical Structure

CAS No. : 854381-37-6

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Esculeogenin A Related Antibodies

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Description

Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia[1][2][3].

IC50 & Target[1]

ACAT-1

 

ACAT-2

 

PPARα

 

NF-κB

 

In Vitro

Esculeogenin A (24 h) dose-dependently inhibits acetyl-LDL-induced cholesterol ester accumulation (but not triglyceride accumulation) in human monocyte-derived macrophages without inducing cytotoxicity[2].
Esculeogenin A (5 h) does not inhibit the association or degradation of acetyl-LDL in human monocyte-derived macrophages[2].
Esculeogenin A (24 h) dose-dependently inhibits cholesterol ester accumulation in Chinese hamster ovary cells overexpressing human ACAT-1 or human ACAT-2 without inducing cytotoxicity[2].
Esculeogenin A (15 min) dose-dependently inhibits ACAT activity in microsomes from human monocyte-derived macrophages, Chinese hamster ovary cells overexpressing human ACAT-1, and Chinese hamster ovary cells overexpressing human ACAT-2, with 50 μmol/L inhibiting HMDM ACAT activity by 40%[2].
Esculeogenin A (24 h) dose-dependently reduces ACAT-1 protein expression in human monocyte-derived macrophages without altering the expression of SR-A or SR-BI[2].
Esculeogenin A (10-100 μM; 24 h) potently inhibits cholesterol ester accumulation in human monocyte-derived macrophages (HMDMs) in a dose-dependent manner without affecting acetyl-LDL uptake or degradation, with 50 μM reducing accumulation by 40%[3].
Esculeogenin A (10-100 μM; 24 h) dose-dependently inhibits cholesterol ester accumulation in both hACAT-1 CHO cells and hACAT-2 CHO cells[3].
Esculeogenin A (10-100 μM) dose-dependently inhibits ACAT activity in human monocyte-derived macrophages (HMDMs), hACAT-1 CHO cells, and hACAT-2 CHO cells[3].
Esculeogenin A (10-50 μM; 24 h) dose-dependently reduces ACAT-1 protein expression in human monocyte-derived macrophages (HMDMs) without altering SR-A or SR-BI expression[3].

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

Esculeogenin A Related Antibodies

Western Blot Analysis[3]

Cell Line: human monocyte-derived macrophages (HMDMs)
Concentration: 10, 30, 50 μM
Incubation Time: 24 h
Result: Reduced ACAT-1 protein expression in HMDMs in a dose-dependent manner.
Left SR-A and SR-BI protein expression unchanged relative to controls.
In Vivo

Esculeogenin A (50-200 mg/kg; p.o.; daily; 12 weeks) dose-dependently alleviates nonalcoholic fatty liver disease in HFD-fed rats by normalizing liver enzyme and lipid levels, improving liver histology, activating the Nrf2 antioxidant pathway, inhibiting NF-κB-mediated inflammation, and regulating hepatic lipogenesis and fatty acid oxidation, with the 200 mg/kg dose fully restoring most parameters to control levels[1].
Esculeogenin A (100 mg/kg/day; p.o.; daily; 90 days), produced in vivo from orally administered Esculeoside A (HY-N18067), is detectable in the aortas of apoE-deficient mice[3].

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

Animal Model: Wistar (male, 10-11 weeks old, ~165 g initial weight, HFD-induced)[1]
Dosage: 50 mg/kg; 100 mg/kg; 200 mg/kg
Administration: p.o.; daily; 12 weeks
Result: Dose-dependently reduced serum ALT, AST, GGT, serum/hepatic TGs, CHOL, LDL-c, liver weight/liver-to-body weight ratio, NF-κB nuclear activity, IKKβ activity, hepatic MDA, IL-6, TNF-α, and hepatic SREBP1, ACC mRNA.
Dose-dependently increased hepatic Nrf2 (mRNA, cytoplasmic, nuclear), GSH, SOD, CAT, HO-1, and hepatic PPARα, CPT I mRNA.
Dose-dependently reduced hepatocellular fat vacuoles and improved liver structure.
200 mg/kg reduced serum/hepatic TGs, CHOL, serum LDL-c in normal diet-fed rats, with no adverse effects on body weight, fat pad weight, or glucose/insulin parameters.
Animal Model: C57BL/6.KOR-Apoeshl (apoE-deficient)[2]
Dosage: 50 mg/kg/day; 100 mg/kg/day (as esculeoside A, converted in vivo to esculeogenin A)
Administration: p.o.; daily; 90 days
Result: Reduced serum total cholesterol by approximately 25%, serum LDL cholesterol by approximately 25%, and serum triglycerides by approximately 45%.
Reduced total aortic surface atherosclerotic lesions to 8.2%.
Reduced aortic sinus cross-sectional lesion area by 52%.
Was detected in the aortas of treated mice, confirming in vivo conversion from Esculeoside A.
Molecular Weight

447.65

Formula

C27H45NO4
CAS No.
SMILES

C[C@@H]1[C@@]2([C@@H](C[C@@H](CN2)CO)O)O[C@]3([H])[C@@]1([H])[C@@]4([C@@]([C@@]5([H])[C@]([C@@]6([C@@](C[C@H](CC6)O)([H])CC5)C)([H])CC4)([H])C3)C
Structure Classification
Initial Source
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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Esculeogenin A Related Classifications

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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:

Esculeogenin A854381-37-6Drug DerivativeAcyltransferaseNF-κBPPARFatty Acid Synthase (FASN)Keap1-Nrf2Drug derivativeDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseNuclear factor-κBNuclear factor-kappaBPeroxisome proliferator-activated receptorsnuclear factor kappa B kinase subunit betahuman monocyte-derived macrophagesapoE-deficient micecarnitine palmitoyltransferase Iacetyl-CoA carboxylasenuclear factor erythroid 2-related factor 2nuclear factor-kappa betaChinese hamster ovary cellsperoxisome proliferator-activated receptor αsterol regulatory element-binding protein 1Inhibitorinhibitorinhibit

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