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primary human hepatocytes

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

4

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137397
    8-Hydroxyefavirenz

    8-OH-EFV

    		 Apoptosis JNK Cancer
    8-Hydroxyefavirenz (8-OH-EFV) is a primary metabolite of (HY-10572). 8-Hydroxyefavirenz induces apoptosis via a JNK- and BimEL-dependent mechanism in primary human hepatocytes. 8-Hydroxyefavirenz can be used in research of cancer . 8-Hydroxyefavirenz is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    8-Hydroxyefavirenz
  • HY-177022
    ALG-001075

    		HBV Infection
    ALG-001075, a capsid assembly modulator (CAM), is an orally active HBV inhibitor. ALG-001075 effectively blocks not only HBV DNA production but also extracellular HBsAg/HBeAg and intracellular HBV RNA in primary human hepatocytes. ALG-001075 shows pronounced reductions of circulating HBV DNA in the AAV-HBV mouse model. ALG-001075 can be used for the study of Chronic hepatitis B (CHB) .
    ALG-001075
  • HY-12281
    FPH2

    BRD-9424

    		 Mitochondrial Metabolism Metabolic Disease Cancer
    FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.
    FPH2
  • HY-100590
    FPH1

    BRD6125

    		 Cytochrome P450 Others
    FPH1(BRD-6125) increases the number and activity of primary human hepatocytes in vitro and promotes the differentiation of iPS cells towards a hepatic lineage .
    FPH1
  • HY-110134
    S07662

    		Constitutive Androstane Receptor Metabolic Disease
    S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC50 of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .
    S07662
  • HY-173465
    DL5055

    		Constitutive Androstane Receptor Metabolic Disease Cancer
    DL5055 (compound 6k) is a potent and selective hCAR activator with an EC50 of 0.35 μM. DL5055 induces CYP2B6 expression and hCAR nuclear translocation in human primary hepatocytes .
    DL5055
  • HY-155108
    OATD-02

    		Arginase Cancer
    OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
    OATD-02
  • HY-173278
    AIC263282

    		HBV Potassium Channel Infection
    AIC263282 is a potent Hepatitis B Virus (HBV) capsid assembly modulator with an EC50 of 3.8 nM. AIC263282 shows an IC50 of 61 nM for hERG. AIC263282 exhibits activity against viral replication and hepatitis B surface antigen (HBsAG) on primary human hepatocytes .
    AIC263282
  • HY-113820
    AZD4619

    		PPAR Metabolic Disease
    AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug .
    AZD4619
  • HY-162738
    JMV6944

    		Cytochrome P450 Ligands for Target Protein for PROTAC Cancer
    JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC50 of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704) .
    JMV6944
  • HY-108614
    GPi688

    		Phosphorylase Metabolic Disease
    GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively . GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia .
    GPi688
  • HY-18056
    PF-915275

    		11β-HSD Metabolic Disease
    PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
    PF-915275
  • HY-155108B
    OATD-02 hydrochloride
    1 Publications Verification

    		 Arginase Cancer
    OATD-02 hydrochloride is the hydrochloride salt form of OATD-02 (HY-155108). OATD-02 hydrochloride an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 hydrochloride bolishes tumor immunosuppression induced by both arginases. OATD-02 hydrochloride can be used for melanoma study .
    OATD-02 hydrochloride
  • HY-14391
    PSI-353661

    GS-558093

    		 HCV Infection
    PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes .
    PSI-353661
  • HY-N2334
    Glycochenodeoxycholic acid
    4 Publications Verification

    Chenodeoxycholylglycine

    		 Endogenous Metabolite Apoptosis STAT BCL6 Interleukin Related Caspase Metabolic Disease Cancer
    Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
    Glycochenodeoxycholic acid
  • HY-18056R
    PF-915275 (Standard)

    		11β-HSD Metabolic Disease
    PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
    PF-915275 (Standard)
  • HY-N2334A
    Glycochenodeoxycholic acid sodium salt
    4 Publications Verification

    Chenodeoxycholylglycine sodium salt; Sodium glycochenodeoxycholate

    		 Endogenous Metabolite Apoptosis STAT BCL6 Interleukin Related Caspase Metabolic Disease Cancer
    Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
    Glycochenodeoxycholic acid sodium salt
  • HY-173391
    4-Hydroxy nonenal glutathione TFA

    4-HNE-GSH TFA

    		 Drug Metabolite Metabolic Disease
    4-Hydroxy nonenal glutathione (4-HNE-GSH) TFA is the primary metabolite of 4-Hydroxy-2-nonenal. 4-Hydroxy nonenal glutathionea TFA is a marker of oxidative stress in rat liver and hepatocytes. 4-Hydroxy nonenal glutathione TFA efficiently prevents formation of DNA adducts with 4-Hydroxy-2-nonenal in human cells .
    4-Hydroxy nonenal glutathione TFA
  • HY-174443
    PROTAC sEH degrader-2

    		PROTACs Epoxide Hydrolase Neurological Disease Inflammation/Immunology
    PROTAC sEH degrader-2 is a PROTAC targeting degradation agent for soluble epoxide hydrolase (sEH) with pIC50 values of the catalytic domain of 8.37 (human sEH-H) and 7.12 (mouce sEH-H). PROTAC sEH degrader-2 can be used for the research related to inflammation and neuroinflammation, such as Alzheimer's disease . (Structure Note: Pink: sEH-H ligand (HY-174225); Blue: CRBN Ligand (HY-103597); E3 + linker (HY-141011))
    PROTAC sEH degrader-2
  • HY-148780
    HBV-IN-29

    		HBV Infection
    HBV-IN-29 (ex8), a flavone derivative, is a potent covalently closed circular DNA (cccDNA) inhibitor. cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-29 has the potential for the research of HBV infection .
    HBV-IN-29
  • HY-148781
    HBV-IN-30

    		HBV Infection
    HBV-IN-30 (ex44), a flavone derivative, is a potent covalently closed circular DNA (cccDNA) inhibitor. cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-30 has the potential for the research of HBV infection .
    HBV-IN-30
  • HY-N2334R
    Glycochenodeoxycholic acid (Standard)

    Chenodeoxycholylglycine (Standard)

    		 Reference Standards Endogenous Metabolite Apoptosis STAT BCL6 Interleukin Related Caspase Metabolic Disease Cancer
    Glycochenodeoxycholic acid (Standard) is the analytical standard of Glycochenodeoxycholic acid. This product is intended for research and analytical applications. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC)[1][2][3][4].
    Glycochenodeoxycholic acid (Standard)
  • HY-138813R
    N-Desethyl Sunitinib hydrochloride (Standard)

    SU-12662 hydrochloride (Standard)

    		 Reference Standards Drug Metabolite Cancer
    Glycochenodeoxycholic acid sodium salt (Standard) is the analytical standard of Glycochenodeoxycholic acid sodium salt. This product is intended for research and analytical applications. Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
    N-Desethyl Sunitinib hydrochloride (Standard)
  • HY-N2334AR
    Glycochenodeoxycholic acid sodium salt (Standard)

    Chenodeoxycholylglycine sodium salt (Standard); Sodium glycochenodeoxycholate (Standard)

    		 Reference Standards Endogenous Metabolite Apoptosis STAT BCL6 Interleukin Related Caspase Metabolic Disease Cancer
    Glycochenodeoxycholic acid sodium salt (Standard) is the analytical standard of Glycochenodeoxycholic acid sodium salt. This product is intended for research and analytical applications. Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
    Glycochenodeoxycholic acid sodium salt (Standard)
  • HY-173033
    MI-883

    		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 .
    MI-883

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