2. Search Result
Search Result
Results for "

hepatocyte microsomes

" in MedChemExpress (MCE) Product Catalog:

26

Inhibitors & Agonists

1

Biochemical Assay Reagents

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109171
    Elinzanetant

    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-149055
    ACT-777991

    		CXCR Inflammation/Immunology
    ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11 .
    ACT-777991
  • HY-160023
    Elisrasib

    D3S-001

    		 Ras PERK Cancer
    Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    Elisrasib
  • HY-122616
    PF-06273340

    		Trk Receptor Neurological Disease
    PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
    PF-06273340
  • HY-145154
    Digoxigenin monodigitoxoside

    		Na+/K+ ATPase Drug Metabolite Cardiovascular Disease Metabolic Disease
    Digoxigenin monodigitoxoside, a metabolite of Digoxin (HY-B1049), belongs to the class of cardenolides. Digoxigenin monodigitoxoside exerts its function by inhibiting Na,K-ATPase. Digoxigenin monodigitoxoside is used for the research of cardiovascular diseases such as congestive heart failure and cardiac arrhythmias .
    Digoxigenin monodigitoxoside
  • HY-19400
    DPC-681

    DPH-153893

    		 HIV Protease HIV Cytochrome P450 Infection
    DPC-681 (DPH-153893) is an orally active HIV inhibitor. DPC-681 inhibits HIV protease activity and inhibits wild-type and mutant HIV replication. DPC-681 can be used for the research of HIV infection .
    DPC-681
  • HY-109173
    Filapixant

    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-W795960
    D-myo-Inositol 1,4,5-trisphosphate sodium salt

    		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-106379
    Lurosetron

    GR-87442

    		 5-HT Receptor Neurological Disease
    Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM. .
    Lurosetron
  • HY-15042
    MK 0686

    		Bradykinin Receptor Metabolic Disease
    MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
    MK 0686
  • HY-168956
    Pks13-IN-2

    		Bacterial Infection
    Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 shows good metabolic stability in mouse liver microsomes and hepatocytes. Pks13-IN-2 can be used for tuberculosis research .
    Pks13-IN-2
  • HY-N11827
    Isocorybulbine

    (+)-Isocorybulbine

    		 Drug Metabolite Inflammation/Immunology
    Isocorybulbine ((+)-Isocorybulbine) is one of the main metabolites of Corydaline (HY-N0923) in human liver microsomes and liver cells. Corydaline has anti-acetylcholinesterase, anti-allergic, anti-allergic reaction and gastric emptying activities. Isocorybulbine can be used for the metabolic study of Corydaline .
    Isocorybulbine
  • HY-162074
    Nipamovir

    		HIV Infection
    Nipamovir is an orally active anti-HIV prodrug. Nipamovir is cleaved in vivo by glutathione and other active thiols. Nipamovir inhibits the replication of HIV-1RF and HIV-192HT599 in cells, with EC50 values of 3.64 μM and 3.23 μM, respectively. Nipamovir can be used in studies related to HIV infection .
    Nipamovir
  • HY-183267
    ERAP1-IN-4

    		Aminopeptidase Cancer
    ERAP1-IN-4 is an orally acvtive endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with a pIC50 of 7.9 and an LLE of 5.3. ERAP1-IN-4 inhibits hydrolysis of peptide substrates by ERAP1, with high activity against Allotype1 and Allotype2. ERAP1-IN-4 reduced efficacy against other allotypes, and modulates ERAP1-mediated peptide processing to inhibit antigenic epitope presentation. ERAP1-IN-4 can be used for the research of cancer[1].
    ERAP1-IN-4
  • HY-181543
    CVN14

    		CD38 Neurological Disease
    CVN14 is a potent, selective and brain-penetrant CD38 inhibitor with human IC50 19 nM, mouse IC50 2.4 nM. CVN14 binds uncompetitively to form a complex with CD38 and ADPR, and inhibits CD38 enzymatic activity. CVN14 can be used for the research of neurodegenerative diseases .
    CVN14
  • HY-181983
    VPC285785

    		SARS-CoV Infection
    VPC285785 is an orally active SARS-CoV-2 main protease inhibitor with an IC50 of 0.8 μM and a Kd of 2.7 μM. VPC285785 functionally inhibits the viral main protease-mediated processing of viral polyprotein precursors required for viral replication. VPC285785 reduces viral loads in the liver, brain and spleen tissues of MHV-infected mice. VPC285785 is applicable to the research of coronavirus infections .
    VPC285785
  • HY-181488
    NLRP3-IN-87

    		NOD-like Receptor (NLR) Caspase Interleukin Related Metabolic Disease Inflammation/Immunology
    NLRP3-IN-87 is a selective and orally active NLRP3 inhibitor with a Kd of 0.23 μM. NLRP3-IN-87 binds directly to the NLRP3 NACHT domain, disrupts NLRP3-NEK7 and NLRP3-ASC interactions, inhibits ASC oligomerization, and blocks inflammasome assembly. NLRP3-IN-87 suppresses caspase-1 activation and IL-1β secretion. NLRP3-IN-87 exhibits anti-inflammatory and analgesic activity, reducing joint swelling, inflammation, and pain in an MSU (HY-B2130A)-induced acute gout mouse model. NLRP3-IN-87 can be used for the research of gout .
    NLRP3-IN-87
  • HY-W663179
    DNDI-VL-2098

    		Parasite Cytochrome P450 Infection
    DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .
    DNDI-VL-2098
  • HY-183709
    Nav1.8-IN-24

    		Sodium Channel Neurological Disease
    Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain .
    Nav1.8-IN-24
  • HY-156957
    5-CNAC disodium

    		Biochemical Assay Reagents Others
    5-CNAC disodium is an orally active enhancer of absorption, with no pharmacological activity on its own. 5-CNAC disodium can significantly enhance the absorption efficiency of the drug (such as Salmon calcitonin (HY-P0090)) when administered together with it in the gastrointestinal tract. 5-CNAC disodium binds reversibly and non-covalently to peptide drugs, protecting them from degradation by gastrointestinal enzymes, increasing their lipid solubility, promoting passive transcellular absorption, and not damaging the integrity of the intestinal epithelium. 5-CNAC disodium can be used in the research of adjuvants for orally administered peptide agents .
    5-CNAC disodium
  • HY-W237019
    3-Ethoxybenzamide

    		Bacterial Infection
    3-Ethoxybenzamide is an alkoxybenzamide compound with antibacterial activity and a FtsZ inhibitor that can cross the blood-brain barrier. 3-Ethoxybenzamide distributes widely and rapidly in vivo, rapidly reaches equilibrium between various tissues and blood, and is linearly taken up by hepatocytes. 3-Ethoxybenzamide is completely dependent on hepatic microsomal oxidation for clearance, with salicylamide as its major metabolite. 3-Ethoxybenzamide can be used for the study of bacterial infections .
    3-Ethoxybenzamide
  • HY-112481
    IKK2-IN-5

    		Inflammation/Immunology
    IKK2-IN-5 is a selective IKK-2 inhibitor with an IC50 of 0.025 μM. IKK2-IN-5 inhibits the production of TNF-α in LPS (HY-D1056)-stimulated human peripheral blood mononuclear cells. IKK2-IN-5 exhibits extremely low cytotoxicity against human peripheral blood mononuclear cells .
    IKK2-IN-5
  • HY-182357
    PAK1-IN-3

    		PAK Potassium Channel Others
    PAK1-IN-3 is a PAK1 inhibitor with an IC50 of 10 nM, an IC50 of 20 nM against PAK2, and an IC50 of 1079 nM against hERG potassium channels. PAK1-IN-3 forms a salt bridge with Asp106 in PAK1 via a properly positioned tertiary amine. PAK1-IN-3 inhibits PAK2 and hERG potassium channels .
    PAK1-IN-3
  • HY-182697
    RTICBM-74

    		Cannabinoid Receptor Metabolic Disease
    RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .
    RTICBM-74
  • HY-182905
    SSTR5/TGR5-modulator-1

    		Somatostatin Receptor G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .
    SSTR5/TGR5-modulator-1
  • HY-N17495
    Luteolin 7-O-(6-O-malonyl-β-D-glucoside)

    		Others Metabolic Disease
    Luteolin 7-O-(6-O-malonyl-β-D-glucoside) is an orally active flavonoid free radical scavenger. Luteolin 7-O-(6-O-malonyl-β-D-glucoside) scavenges free radicals, inhibits the activity elevation of aspartate aminotransferase and alanine aminotransferase in mouse plasma, as well as the elevation of liver lipid hydroperoxide content. Luteolin 7-O-(6-O-malonyl-β-D-glucoside) is applicable for liver injury research .
    Luteolin 7-O-(6-O-malonyl-β-D-glucoside)

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: