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hepatocyte receptors

" in MedChemExpress (MCE) Product Catalog:

91

Inhibitors & Agonists

1

Biochemical Assay Reagents

3

Peptides

5

Inhibitory Antibodies

10

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4

Isotope-Labeled Compounds

4

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15424
    5-Iodotubercidin
    10+ Cited Publications

    NSC 113939; 5-ITu

    Adenosine Kinase Cancer
    5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
    5-Iodotubercidin
  • HY-B0144A
    Pitavastatin
    10+ Cited Publications

    NK-104

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects .
    Pitavastatin
  • HY-B0144
    Pitavastatin Calcium
    10+ Cited Publications

    NK-104 hemicalcium; Pitavastatin hemicalcium

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin Calcium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects .
    Pitavastatin Calcium
  • HY-112540B

    Endogenous Metabolite Metabolic Disease
    Acetoacetic acid sodium is an oxidative stress inducer that affects the antioxidant enzyme system and lipoprotein metabolism. Acetoacetic acid sodium induces oxidative stress by decreasing the mRNA expression and activity of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px), increasing MDA content, and inhibiting very low density lipoprotein (VLDL) assembly by downregulating apolipoprotein ApoB100, ApoE, and low density lipoprotein receptor (LDLR), leading to triglyceride (TG) accumulation in hepatocytes. Acetoacetic acid sodium can be used to study metabolic diseases .
    Acetoacetic acid sodium
  • HY-P99391

    ABT-700; ABBV-400 Antibody

    c-Met/HGFR Apoptosis Cancer
    Telisotuzumab (ABT-700) is a bivalent humanized IgG1 anti-c-Met monoclonal antibody. Telisotuzumab binds cellular c-Met and disrupts its productive dimerization and activation induced by HGF or by the high density of c-Met on the cell surface independent of ligand. Telisotuzumab induces apoptosis. Telisotuzumab can be used for the study of cancers harboring amplified MET, such as gastric and lung cancers .
    Telisotuzumab
  • HY-103243
    TCPOBOP
    4 Publications Verification

    Bcl-2 Family Cancer
    TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss . TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins .
    TCPOBOP
  • HY-112540
    Acetoacetic acid
    4 Publications Verification

    Endogenous Metabolite Metabolic Disease
    Acetoacetic acid is an oxidative stress inducer that affects the antioxidant enzyme system and lipoprotein metabolism. Acetoacetic acid induces oxidative stress by decreasing the mRNA expression and activity of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px), increasing MDA content, and inhibiting very low density lipoprotein (VLDL) assembly by downregulating apolipoprotein ApoB100, ApoE, and low density lipoprotein receptor (LDLR), leading to triglyceride (TG) accumulation in hepatocytes. Acetoacetic acid can be used to study metabolic diseases .
    Acetoacetic acid
  • HY-109171

    NT-814; BAY3427080

    Neurokinin Receptor Cardiovascular Disease Neurological Disease
    Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
    Elinzanetant
  • HY-12423

    TAS-115

    VEGFR c-Met/HGFR Cancer
    Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
    Pamufetinib
  • HY-148118A

    LYTACs Cancer
    Tri-GalNAc(OAc)3 TFA is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3 TFA can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
    Tri-GalNAc(OAc)3 TFA
  • HY-113422

    Endogenous Metabolite Glucocorticoid Receptor Inflammation/Immunology
    Tetrahydrocorticosterone is a glucocorticoid. One of its active forms, 5α-Tetrahydrocorticosterone (HY-113364), exerts its effects by binding to the GC receptor and inhibiting inflammatory processes. Tetrahydrocorticosterone is naturally synthesized by the adrenal glands and plays a key role in regulating the metabolism of carbohydrates, proteins and fats .
    Tetrahydrocorticosterone
  • HY-W013150

    GABA Receptor Neurological Disease
    Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions .
    Alpidem
  • HY-16969
    Dihexa
    5+ Cited Publications

    PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2

    c-Met/HGFR Neurological Disease
    Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
    Dihexa
  • HY-137455

    ANG-3777

    c-Met/HGFR Inflammation/Immunology
    Terevalefim (ANG-3777), an hepatocyte growth factor (HGF) mimetic, selectively activates the c-Met receptor .
    Terevalefim
  • HY-B0822

    Environmental Pollutants Cytochrome P450 GABA Receptor Apoptosis Neurological Disease
    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 .
    Fipronil
  • HY-112540A
    Acetoacetic acid lithium
    4 Publications Verification

    Endogenous Metabolite Metabolic Disease
    Acetoacetic acid lithium is an oxidative stress inducer that affects the antioxidant enzyme system and lipoprotein metabolism. Acetoacetic acid lithium induces oxidative stress by decreasing the mRNA expression and activity of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px), increasing MDA content, and inhibiting very low density lipoprotein (VLDL) assembly by downregulating apolipoprotein ApoB100, ApoE, and low density lipoprotein receptor (LDLR), leading to triglyceride (TG) accumulation in hepatocytes. Acetoacetic acid lithium can be used to study metabolic diseases .
    Acetoacetic acid lithium
  • HY-N2078

    Neodiosgenin

    LXR Reactive Oxygen Species (ROS) Apoptosis Fatty Acid Synthase (FASN) Metabolic Disease
    Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC50 of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer .
    Yamogenin
  • HY-G0007
    Omeprazole sulfone
    2 Publications Verification

    Omeprazole sulphone

    Drug Metabolite Cytochrome P450 Aryl Hydrocarbon Receptor Inflammation/Immunology
    Omeprazole sulfone (Omeprazole sulphone) is one of the major circulating metabolites of Omeprazole (HY-B0113) in vivo, and belongs to class 4 non-mutagenic impurities. Omeprazole sulfone does not bind to the aryl hydrocarbon receptor (AhR), nor does it induce the expression of CYP1A1 or CYP1A2. However, Omeprazole sulfone promotes the migration of gastric epithelial cells under basal conditions and reverses the inhibitory effect of Indomethacin (HY-14397) on cell migration. Omeprazole sulfone does not promote cell proliferation, nor does it upregulate COX-2 expression or activate signaling pathways such as ERK, P38 MAPK and PI3K. Omeprazole sulfone maintains basal ulcer healing under non-acid-dependent conditions and can be used in studies related to gastric ulcer repair .
    Omeprazole sulfone
  • HY-168046

    Thyroid Hormone Receptor Metabolic Disease
    ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC50 of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease .
    ALG-055009
  • HY-G0006
    Omeprazole sulfide
    2 Publications Verification

    Ufiprazole

    Drug Metabolite Aryl Hydrocarbon Receptor Bacterial Infection Metabolic Disease
    Omeprazole sulfide (Ufiprazole) is a metabolic degradation product of Omeprazole (HY-B0113). Omeprazole sulfide acts as a modulator of AhR. Omeprazole sulfide in cells with low CYP3A4 expression, functions as an AhR antagonist; however, in cells with high CYP3A4 expression, it is rapidly metabolized to Omeprazole, thereby acting as an AhR agonist. Omeprazole sulfide exhibits antibacterial activity when conjugated with silver nanoparticles (AgNPs). Omeprazole sulfide can be used in research on acid suppression and bacterial infections .
    Omeprazole sulfide
  • 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 .
    Ficlatuzumab
  • HY-132814

    ATH-1017

    c-Met/HGFR Neurological Disease
    Fosgonimeton (ATH-1017) is a hepatocyte growth factor receptor (c-Met/HGFR) agonist. Fosgonimeton has neuroprotective effects in both LPS (HY-D1056) -induced neuroinflammation and Aβ-induced AD models .
    Fosgonimeton
  • HY-132590A

    ALN-TTRSC sodium

    Small Interfering RNA (siRNA) Transthyretin (TTR) Neurological Disease
    Revusiran (ALN-TTRSC) sodium is an RNA interference agent targeting the mRNA of transthyretin (Transthyretin, TTR). Revusiran sodium mediates sequence-specific degradation of TTR mRNA through RNA interference, reduces the synthesis of TTR protein, binds to GalNAc ligands, and is taken up by hepatocytes via the asialoglycoprotein receptor. Revusiran sodium exhibits favorable nonclinical safety profiles. Revusiran sodium can be used in studies related to transthyretin-mediated amyloidosis .
    Revusiran sodium
  • HY-12423A

    TAS-115 mesylate

    VEGFR c-Met/HGFR Cancer
    Pamufetinib (TAS-115) mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
    Pamufetinib mesylate
  • HY-B0822R

    Reference Standards GABA Receptor Cytochrome P450 Apoptosis Neurological Disease
    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 .
    Fipronil (Standard)
  • HY-139787A

    ISIS-721744; IONIS-PKK-LRX

    Kallikrein Cardiovascular Disease Inflammation/Immunology
    Donidalorsen (ISIS-721744; IONIS-PKK-LRX) sodium is an antisense oligonucleotide targeting prekallikrein (PKK). Donidalorsen sodium inhibits kallikrein activity and reduces the production of Bradykinin (HY-P0206) by specifically binding to and degrading PKK mRNA in the liver. Donidalorsen sodium can be used in the research of hereditary angioedema .
    Donidalorsen sodium
  • HY-P1415A
    Norleual TFA
    1 Publications Verification

    c-Met/HGFR Angiotensin Receptor Cardiovascular Disease Neurological Disease Metabolic Disease
    Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
    Norleual TFA
  • HY-153184

    Asialoglycoprotein Receptor (ASGPR) Small Interfering RNA (siRNA) Metabolic Disease
    GalNAc-L96 free base is a conjugate of GalNAc and its ligand L96. When conjugated with the A-rich HCV sequence (H12), GalNAc-L96 free base binds potently to ASGPR, with a Ki value of 10.4 nM. GalNAc-L96 free base promotes siRNA delivery to hepatocytes .
    GalNAc-L96 free base
  • HY-113364

    5α-THB

    Glucocorticoid Receptor Endogenous Metabolite Drug Metabolite Metabolic Disease Inflammation/Immunology
    5α-Tetrahydrocorticosterone (5α-HB), an endogenous steroid, is a glucocorticoid receptor (GR) agonist and a metabolite of Corticosterone (HY-B1618). 5α-Tetrahydrocorticosterone is an effective topical anti-inflammatory agent in vivo. 5α-Tetrahydrocorticosterone reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a Kd of 268 nM. 5α-Tetrahydrocorticosterone can be used for research on inflammatory skin diseases .
    5α-Tetrahydrocorticosterone
  • HY-109173

    BAY 1902607

    P2X Receptor Cytochrome P450 Inflammation/Immunology
    Filapixant (BAY 1902607) is an orally active and selective P2X3 receptor antagonist. Filapixant is applicable to the research of refractory chronic cough .
    Filapixant
  • HY-W587772

    MEHHTP

    Drug Metabolite Metabolic Disease
    Mono (2-ethyl-5-hydroxyhexyl) terephthalate (MEHHTP), a hydroxyl metabolite of the phthalate alternative Di-2-ethylhexyl terephthalate (DEHTP), is a liver X receptor α (LXRα) agonist with a binding energy of -7.41 kcal/mol. Mono (2-ethyl-5-hydroxyhexyl) terephthalate upregulates LXRα downstream targets such as SREBP-1c and FASN and increases lipogenic enzyme activity in hepatocytes, and elevating triglyceride (TG) levels. Mono (2-ethyl-5-hydroxyhexyl) terephthalate is promising for research of nonalcoholic fatty liver disease (NAFLD) .
    Mono(2-ethyl-5-hydroxyhexyl) terephthalate
  • HY-149056

    MAP4K Interleukin Related Cancer
    GNE-6893 is an orally active, selective HPK1 inhibitor with a Ki < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers .
    GNE-6893
  • HY-N3741

    Didrovaltratum

    Calcium Channel Reactive Oxygen Species (ROS) Autophagy Inflammation/Immunology Cancer
    Didrovaltrate (Didrovaltratum) is an L-type calcium channel blocker, ROS scavenger, autophagy enhancer, and lipid accumulation inhibitor. Didrovaltrate blocks L-type calcium currents in a concentration-dependent manner, shifts the current-voltage curve upward, modulates steady-state inactivation kinetics, and inhibits the nuclear translocation of glucocorticoid receptors. Didrovaltrate reduces ROS levels, downregulates the expression of muscle atrophy-related genes, enhances autophagy via lipophagy, and decreases Oleic acid-induced lipid accumulation. Didrovaltrate exhibits cytotoxic activity against cancer cells. Didrovaltrate can be used in research related to skeletal muscle atrophy, non-alcoholic fatty liver disease, breast cancer, lung cancer, gastric cancer, and prostate cancer .
    Didrovaltrate
  • HY-135319

    Bacterial Antibiotic ERK JNK NF-κB ROR Apoptosis Caspase GSK-3 Akt PI3K Infection Metabolic Disease Inflammation/Immunology Cancer
    Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .
    Strictinin
  • HY-156897

    Drug-Linker Conjugates for ADC Cancer
    Val-Cit-amide-Ph-Maytansine is an antibody and bispecific antigen-binding mol. that bind hepatocyte growth factor receptor c-Met (MET) or antibody-drug conjugates (ADCs) .
    Val-Cit-amide-Ph-Maytansine
  • HY-113820

    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-B0144AS1

    NK-104-d5 sodium

    Apoptosis HMG-CoA Reductase (HMGCR) Mitophagy Autophagy Metabolic Disease Cancer
    Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
    Pitavastatin-d5 sodium
  • HY-B0144B

    NK-104 sodium

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects .
    Pitavastatin sodium
  • HY-15424R

    NSC 113939 (Standard); 5-ITu (Standard)

    Adenosine Kinase Reference Standards Cancer
    5-Iodotubercidin (Standard) is the analytical standard of 5-Iodotubercidin. This product is intended for research and analytical applications. 5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
    5-Iodotubercidin (Standard)
  • HY-76520

    IPI 1040; TBC-11251

    Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan
  • HY-W795960

    Biochemical Assay Reagents Calcium Channel Phospholipase Neurological Disease Metabolic Disease
    D-myo-inositol 1,4,5-trisphosphate sodium salt is a widely distributed intracellular second messenger. D-myo-inositol 1,4,5-trisphosphate sodium salt acts as a potent agonist of the Ins (1,4,5) P3 receptor with an EC50 of 0.12 μM and inhibits bovine PLC-δ1, with an IC50 of 5.4 μM for binding and an IC50 of 12.4 μM for hydrolysis. D-myo-inositol 1,4,5-trisphosphate sodium saltis metabolized into Ins (1,4) P2 and Ins (1,3,4,5) P4. D-myo-inositol 1,4,5-trisphosphate sodium salt mediates various cellular processes, including growth, development, fertilization, secretion, contraction and neuromodulation. D-myo-inositol 1,4,5-trisphosphate sodium salt inhibits PIP2 hydrolysis and Ca 2+-ATPase activity. D-myo-inositol 1,4,5-trisphosphate sodium salt is used for cardiac preconditioning, exerts cardioprotective effects and mimics ischemic preconditioning. D-myo-inositol 1,4,5-trisphosphate sodium salt is applied in studies related to intracellular calcium and phosphoinositol signaling pathways .
    D-myo-Inositol 1,4,5-trisphosphate sodium salt
  • HY-132590

    ALN-TTRSC

    Small Interfering RNA (siRNA) Transthyretin (TTR) Neurological Disease
    Revusiran (ALN-TTRSC) is an RNA interference agent targeting the mRNA of transthyretin (Transthyretin, TTR). Revusiran mediates sequence-specific degradation of TTR mRNA through RNA interference, reduces the synthesis of TTR protein, binds to GalNAc ligands, and is taken up by hepatocytes via the asialoglycoprotein receptor. Revusiran exhibits favorable nonclinical safety profiles. Revusiran can be used in studies related to transthyretin-mediated amyloidosis .
    Revusiran
  • HY-170973

    Opioid Receptor
    KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
    KOR agonist 4
  • HY-B0144AR

    NK-104 (Standard)

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Reference Standards Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Pitavastatin (Standard) is the analytical standard of Pitavastatin. This product is intended for research and analytical applications. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects .
    Pitavastatin (Standard)
  • HY-P1415

    c-Met/HGFR Angiotensin Receptor Neurological Disease Metabolic Disease
    Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
    Norleual
  • HY-177134

    VEGFR c-Met/HGFR Cancer
    Taligantinib (Compound Example 70) is an orally active and selective dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). Taligantinib suppresses tumor angiogenesis and cell proliferation. Taligantinib is promising for research of solid tumors such as non-small cell lung cancer and hepatocellular carcinoma .
    Taligantinib
  • HY-P99391A

    ABT-700 (powder)

    c-Met/HGFR Apoptosis Cancer
    Telisotuzumab (ABT-700) (powder) is a bivalent humanized IgG1 anti-c-Met monoclonal antibody. Telisotuzumab (powder) binds cellular c-Met and disrupts its productive dimerization and activation induced by HGF or by the high density of c-Met on the cell surface independent of ligand. Telisotuzumab (powder) induces apoptosis. Telisotuzumab (powder) can be used for the study of cancers harboring amplified MET, such as gastric and lung cancers .
    Telisotuzumab (powder)
  • HY-10338A

    c-Met/HGFR VEGFR Cancer
    Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB .
    Foretinib phosphate
  • HY-B0144S

    NK-104-d4 hemicalcium; Pitavastatin-d4 hemicalcium

    Isotope-Labeled Compounds HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Metabolic Disease Cancer
    Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
    Pitavastatin-d4 hemicalcium
  • HY-B0144AS3

    NK-104-d4-1 sodium

    Isotope-Labeled Compounds HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cardiovascular Disease Neurological Disease Metabolic Disease
    Pitavastatin-d4-1 (NK-104-d4-1) sodium is the deuterium labeled Pitavastatin sodium (HY-B0144B). Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects .
    Pitavastatin-d4-1 sodium

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