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HepaRG

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By Targets:	Akt (1) Apoptosis (3) Constitutive Androstane Receptor (1) Cytochrome P450 (2) Drug Metabolite (1) Keap1-Nrf2 (1) mAChR (1) mTOR (1) PERK (1) Phosphatase (1) PPAR (2) Pregnane X Receptor (PXR) (3) PROTACs (1) Reference Standards (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Infection (1) Metabolic Disease (5) Neurological Disease (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13690

Mitotane 5 Publications Verification 2,4′-DDD; o,p'-DDD	Apoptosis	Cancer
Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions .

HY-173072

SJPYT-310	Pregnane X Receptor (PXR)	Others
SJPYT-310 is a selective PXR antagonist. SJPYT-310 shows no significant cytotoxicity .

HY-W203683

Perfluorononanoic acid PFNA; Heptadecafluorononanoic acid	PPAR PERK	Metabolic Disease
Perfluorononanoic acid (PFNA) is an orally active PPARα activator. Perfluorononanoic acid activates PPARα-mediated gene expression, including upregulating target genes associated with lipid metabolism and triglyceride storage. Perfluorononanoic acid exhibits certain developmental and reproductive toxicity. Perfluorononanoic acid causes hepatomegaly in pregnant mice, induces high postnatal mortality in neonatal mice, and leads to dose-dependent delays in eye-opening time and puberty onset in mouse offspring .

HY-113848

AEM1	Keap1-Nrf2	Cancer
AEM1 is an Nrf2 inhibitor with anti-tumor and oral activity. AEM1 promotes the differentiation of HepaRG cells towards mature liver cells, aiding in the recovery of damaged liver .

HY-175266

MI1013	PROTACs Cytochrome P450 Pregnane X Receptor (PXR)	Metabolic Disease
MI1013 is a PROTAC PXR degrader (DC₅₀ = 89 nM, D_max = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67). (Pink: PXR ligand 3: HY-175267, Blue: Pomalidomide-propargyl ligand: HY-W410002, Pink + Black: PXR ligand-Linker Conjugate 1: HY-175268) .

HY-13690R

Mitotane (Standard) 2,4′-DDD (Standard); o,p'-DDD (Standard)	Reference Standards Apoptosis	Cancer
Mitotane (Standard) is the analytical standard of Mitotane. This product is intended for research and analytical applications. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions .

HY-18203

HBF-0079	Apoptosis Akt mTOR	Cancer
HBF-0079 is a selective anti-hepatocellular carcinoma agent. HBF-0079 induces cell cycle arrest and Apoptosis. HBF-0079 modulates cell-growth and anti-apoptotic signaling through AKT and mTOR. HBF-0079 exhibits antitumor activity against hepatocellular carcinoma .

HY-173033

MI-883	Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450	Metabolic Disease
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC₅₀=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC₅₀=0.1 μM). MI-883 stimulates CAR LBD assembly (EC₅₀=0.38 µM) and CAR3 variant activation (EC₅₀=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC₅₀=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .

HY-N10830

(±)-Nirtetralin	Others	Infection
(±)-Nirtetralin is an isomer of Nirtetralin, which inhibits growth of hepatitis E virus (HEV) in HepaRG cells .

HY-173217

PPARα agonist 5	PPAR Phosphatase	Cardiovascular Disease Metabolic Disease
PPARα agonist 5 is an orally available, selective partial agonist of PPARα (EC₅₀: 3 nM). PPARα agonist 5 reduces lipid accumulation and upregulates key PPARα target genes, exerting anti-fatty liver effects. PPARα agonist 5 also exhibits significant hypolipidemic and hypoglycemic effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) (IC₅₀: 79.1 μM). PPARα agonist 5 has a good safety profile and can be used in the study of type 2 diabetes with dyslipidemia .

HY-W505108

2,3-Dihydroxypropyl pentadecanoate	Drug Metabolite	Metabolic Disease
2,3-Dihydroxypropyl pentadecanoate is a monoacylglycerol that is found in wheat bran extracts. 2,3-Dihydroxypropyl pentadecanoate levels are increased in a HepaRG cell-based model of hepatic steatosis induced by BSA-conjugated palmitate .

HY-181559S

VU6025733 AG06827	mAChR	Neurological Disease
VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M₄ mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC₅₀ of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease .

(±)-Nirtetralin	Phyllanthus urinaria Linn. Lignans Euphorbiaceae Phenylpropanoids Plants Source Classification	Others
(±)-Nirtetralin is an isomer of Nirtetralin, which inhibits growth of hepatitis E virus (HEV) in HepaRG cells .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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HepaRG

Inhibitors & Agonists

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Natural
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