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ADME profiling

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114301
    PF-06305591

    		Sodium Channel Neurological Disease
    PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
    PF-06305591
  • HY-178317
    OUL312

    		PARP Apoptosis Infection Inflammation/Immunology Cancer
    OUL312 is a potent PARP10 inhibitor (IC50 = 20 nM), showing more than 75-fold greater selectivity for PARP15 (IC50 = 1500 nM). OUL312 is also at least 18-fold higher than all other human enzymes in the family. OUL312 has a good ADME profile, is able to enter cells, is not toxic, and effectively rescues human cells from PARP10-induced apoptosis at sub-micromolar concentrations. OUL312 can be used for the study of cervical cancer .
    OUL312
  • HY-114301A
    PF-06305591 dihydrate

    		Sodium Channel Neurological Disease
    PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
    PF-06305591 dihydrate
  • HY-176287
    ARN25657

    		Dopamine Receptor GSK-3 PKA P-glycoprotein Neurological Disease
    ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
    ARN25657
  • HY-139562
    BMS-986318

    		FXR Metabolic Disease
    BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
    BMS-986318
  • HY-155518
    IRAK4-IN-25

    		IRAK Inflammation/Immunology
    IRAK4-IN-25 (compound 38) is an orally acitve and potent IRAK4 inhibitor (IC50=7.3 nM), with low clearance (Cl=12 mL/min/kg). IRAK4-IN-25 inhibits production of pro-inflammatory cytokines, and shows in vitro safety and ADME profiles. IRAK4-IN-25 can be used for research in inflammatory and autoimmune disorders .
    IRAK4-IN-25
  • HY-124364
    RO6889678

    		HBV Cytochrome P450 Infection Metabolic Disease
    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 .
    RO6889678
  • HY-180452
    HAT-IN-10

    		Paraptosis Infection
    HAT-IN-10 (Compound 12a) is an anti-human African trypanosomiasis (HAT) agent, with an EC50 value of 0.23 μM for T. brucei. HAT-IN-10 can be used for research on HAT .
    HAT-IN-10
  • HY-179617
    Cbl-b-IN-30

    		E1/E2/E3 Enzyme Interleukin Related Cancer
    Cbl-b-IN-30 is an orally active Casitas B-lineage lymphoma-b (CBLB) inhibitor. Cbl-b-IN-30 specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity with an IC50 of 9.1 nM. Cbl-b-IN-30 can promote IL-2 secretion (EC50 = 187.5 nM) and enhance T cell activation. Cbl-b-IN-30 exerts antitumor activity and can induce immune memory. Cbl-b-IN-30 can be used for the research of colon cancer .
    Cbl-b-IN-30

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