Search Result
Results for "
Human Hepatocytes
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-137397
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8-OH-EFV
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Apoptosis
JNK
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Cancer
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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.
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- HY-B0822
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GABA Receptor
Cytochrome P450
Apoptosis
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Neurological Disease
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Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .
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- HY-12281
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BRD-9424
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Others
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Metabolic Disease
Cancer
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FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.
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- HY-100590
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BRD6125
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Others
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Others
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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 .
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- HY-112540B
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Endogenous Metabolite
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Metabolic Disease
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Acetoacetic acid sodium is a metabolite of non-esterified fatty acids, involved in the development of human diabetes. Acetoacetic acid sodium induces oxidative stress to inhibit the assembly of very low density lipoprotein in bovine hepatocytes .
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- HY-110134
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Constitutive Androstane Receptor
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Metabolic Disease
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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) .
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- HY-162854
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Acyltransferase
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Metabolic Disease
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Diacylglycerol acyltransferase inhibitor-2 (Example 8) is an inhibitor of Diacylglycerol Acyl Transferase 2 (DGAT2) with an IC50 value of 3.7 nM .
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- HY-N7790
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Others
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Cancer
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Citrusinol is a natural product isolated from D. caudatum. Citrusinol has anticancer activity and inhibits the proliferation and migration of human hepatocytes HepG 2 .
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- HY-N10426
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Glucosidase
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Metabolic Disease
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(+)-Cembrene A (Compound 5) is a α-glucosidase inhibitor with an IC50 of 30.31 μM. (+)-Cembrene A is nontoxic towards human normal hepatocyte (LO2) cells .
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- HY-149392
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HBV
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Infection
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HBV-IN-35 (Compound 88) is a HBV inhibitor. HBV-IN-35 has anti-HBV activities in mouse and human hepatocytes (EC50: 100 nM and 400 nM respectively) .
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- HY-155108
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Arginase
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Cancer
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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 .
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- HY-P99196
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c-Met/HGFR
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Cancer
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Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). Ficlatuzumab blocks the activation of the HGF/c-Met signaling pathway, and inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion .
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- HY-146111
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IRAK
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Cancer
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IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg .
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- HY-128029
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Others
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Metabolic Disease
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Glycogen phosphorylase-IN-1 (Compound 42) is an inhibitor for human liver glycogen phosphorylase (hlGPa) and hepatocyte glycogen-derived glucose production with IC50s of 53 and 380 nM, respectively. Glycogen phosphorylase-IN-1 reveals efficacy towards type 2 diabetes .
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- HY-163131
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Glucosylceramide Synthase (GCS)
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Neurological Disease
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Glucosylceramide synthase-IN-4 (compound 12) is a potent glucosylceramide synthase (GCS) inhibitor, with an IC50 of 6.8 nM. Glucosylceramide synthase-IN-4 shows excellent PK properties and stability in human hepatocytes. Glucosylceramide synthase-IN-4 has good CNS penetration and acceptable PXR selectivity .
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- HY-113820
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PPAR
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Metabolic Disease
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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 .
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- HY-18056
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Others
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Metabolic Disease
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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 .
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- HY-108614
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Others
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Metabolic Disease
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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 .
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- HY-P4672
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GCGR
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Metabolic Disease
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(Met(O)27)-Glucagon (1-29) (human, rat, porcine) is a modified glucagon. (Met(O)27)-Glucagon (1-29) (human, rat, porcine) has the same maximum glucose-synthesizing activity in rat hepatocytes as native glucagon, but it is less potent, suggesting a crucial role of methionine in the binding of glucagon to its hepatic receptor .
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- HY-162738
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Cytochrome P450
Ligands for Target Protein for PROTAC
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Cancer
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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) .
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- HY-145713
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HBV-IN-19
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HBV
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Infection
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GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
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- HY-120103
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Sodium Channel
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Metabolic Disease
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PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism .
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- HY-128103
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GCGR
Adenylate Cyclase
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Metabolic Disease
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Glucagon receptor antagonists-7 (Compound 1) is an antagonist for hGCGR, that inhibits the binding of 125I-labeled glucagon to the human glucagon receptor (hGCGR) with IC50 of 181 nM. Glucagon receptor antagonists-7 activates glucagon-stimulated adenylyl cyclase with a KDB of 81 nM in CHO cell. Glucagon receptor antagonists-7 inhibits glucagon-mediated glycogenolysis in human hepatocytes, and lowers blood glucose levels .
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- HY-163324A
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Cytochrome P450
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Others
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2-Me PeER is a rhodamine dye-based fluorescent probe that detects CYP3A4 activity. In fluorescence-activated cell sorting (FACS) based on CYP3A4 activity, homogeneous and functional human induced pluripotent stem cell (hiPSC)-derived hepatocytes and intestinal epithelial cells can be obtained with the aid of 2-Me PeER .
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- HY-12564
-
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Aurora Kinase
Apoptosis
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Cancer
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Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells .
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- HY-120270
-
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AMPK
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Metabolic Disease
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PF-06679142 (Compound 10) is a potent, orally active AMPK activator with an EC50 of 22 nM against α1β1γ1-AMPK. PF-06679142 can be used for diabetic nephropathy research .
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- HY-155108B
-
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Arginase
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Cancer
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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 .
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- HY-N2334
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Chenodeoxycholylglycine
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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) .
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- HY-N2334A
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Chenodeoxycholylglycine sodium salt; Sodium glycochenodeoxycholate
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Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
|
Metabolic Disease
Cancer
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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) .
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- HY-116282D
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DSS (MW 450000-550000); DXS (MW 450000-550000)
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HIV
Apoptosis
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Others
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Dextran sulfate sodium salt (MW 450000-550000) is a polymer of anhydroglucose with a molecular weight range of 450000-550000. Dextran sulfate sodium salt (MW 450000-550000) can effectively enrich precipitated cells and can be used to isolate neutrophils from human and rat blood. Dextran sulfate sodium salt (average MW 500000) can effectively enhance the conversion activity of coagulation factor XIIa (FXIIa) to induce hepatocyte growth factor (HGF) and increase the specific activity of FXIIa.
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- HY-124364
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HBV
Cytochrome P450
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Infection
Metabolic Disease
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RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .
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- HY-14391
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GS-558093
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HCV
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Infection
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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 .
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- HY-145713A
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HBV-IN-19 TFA
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HBV
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Infection
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GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
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- HY-148781
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HBV
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Infection
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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 .
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- HY-148780
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HBV
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Infection
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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 .
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- HY-N2334AR
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Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
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Metabolic Disease
Cancer
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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) .
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- HY-B0766
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SY801
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Autophagy
Apoptosis
HBV
HCV
HSP
Reactive Oxygen Species
Bcl-2 Family
Glutathione S-transferase
p38 MAPK
NF-κB
Microtubule/Tubulin
ERK
JNK
TNF Receptor
Interleukin Related
CDK
Cyclin G-associated Kinase (GAK)
mTOR
P-glycoprotein
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
|
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
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- HY-B0822R
-
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GABA Receptor
Cytochrome P450
Apoptosis
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Neurological Disease
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Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P4672
-
|
GCGR
|
Metabolic Disease
|
(Met(O)27)-Glucagon (1-29) (human, rat, porcine) is a modified glucagon. (Met(O)27)-Glucagon (1-29) (human, rat, porcine) has the same maximum glucose-synthesizing activity in rat hepatocytes as native glucagon, but it is less potent, suggesting a crucial role of methionine in the binding of glucagon to its hepatic receptor .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99196
-
|
c-Met/HGFR
|
Cancer
|
Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). Ficlatuzumab blocks the activation of the HGF/c-Met signaling pathway, and inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion .
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- HY-P99391
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ABT-700
|
Inhibitory Antibodies
|
Cancer
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Telisotuzumab (ABT-700) is a human recombinant bivalent antibody, a therapeutic antibody against the hepatocyte growth factor receptor (MET) that binds c-Met with high affinity and inhibits c-Met signaling. Telisotuzumab has antitumor activity .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-112540B
-
-
-
- HY-N2334
-
-
-
- HY-N2334A
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Chenodeoxycholylglycine sodium salt; Sodium glycochenodeoxycholate
|
Structural Classification
Classification of Application Fields
Source classification
Endogenous metabolite
Disease Research Fields
Steroids
Cancer
|
Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
|
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) .
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- HY-N7790
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-
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- HY-N10426
-
-
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- HY-N2334AR
-
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Structural Classification
Source classification
Endogenous metabolite
Steroids
|
Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
|
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) .
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