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intrinsic+clearance

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137967
    Genistein 7-β-D-Glucuronide

    Genistein 7-O-glucuronide

    		 Drug Metabolite Metabolic Disease
    Genistein 7-β-D-Glucuronide (Genistein 7-O-glucuronide) is the primary phase II metabolite of Genistein (HY-14596) in human and rat hepatocytes. Genistein 7-β-D-Glucuronide undergoes distinct deconjugation in different functional assays. Genistein 7-β-D-Glucuronide is produced via hepatic microsomal glucuronidation and shows a mild age-related increase in intrinsic clearance in male F344 rats. Genistein 7-β-D-Glucuronide can be used for research on metabolism .
    Genistein 7-β-D-Glucuronide
  • HY-175207
    CHI3L1-IN-3

    		Glycosidase Cancer
    CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
    CHI3L1-IN-3
  • HY-162238
    OSM-S-106

    		Parasite Infection
    OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
    OSM-S-106
  • HY-170973
    KOR agonist 4

    		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-178282
    JAK1-IN-19

    		JAK Inflammation/Immunology
    JAK1-IN-19 (Compound 18) is a potent JAK1 inhibitor with IC50s of 0.02, 0.5, 91 and 0.2 nM against JAK1, JAK2, JAK3 and TYK2. JAK1-IN-19 exhibits improved rat and human intrinsic clearance. JAK1-IN-19 can be used for the studies of atopic dermatitis and other autoimmune diseases .
    JAK1-IN-19
  • HY-146111
    IRAK4-IN-13

    		IRAK Cancer
    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 .
    IRAK4-IN-13
  • HY-146113
    IRAK4-IN-15

    		IRAK Cancer
    IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .
    IRAK4-IN-15
  • HY-W413619
    Cipargamin enantiomer

    NITD609 enantiomer; KAE609 enantiomer

    		 Parasite Infection
    Cipargamin enantiomer (NITD609 enantiomer) is a Plasmodium falciparum inhibitor that can be characterized as a spirotetrahydro β-carboline (1S,3R stereoisomer). Cipargamin enantiomer exerts antiplasmodial activity against Plasmodium falciparum strains NF54 (IC50 of 77 nM) and K1. Cipargamin enantiomer displays low liver microsomal intrinsic clearance in mouse and human systems. Cipargamin enantiomer does not inhibit CYP2C9. Cipargamin enantiomer can be used for the research of malaria .
    Cipargamin enantiomer

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