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moderate oral bioavailability

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0717
    Tocofersolan
    5+ Cited Publications

    TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS

    		 Drug Derivative Neurological Disease Metabolic Disease
    Tocofersolan is synthetic polyethylene glycol derivative of α-tocopherol. Tocofersolan is an orally active and water-soluble analog of vitamin E. Tocofersolan can reduce neurobehavioral deficits in zebrafish embryos exposed to moderate and high concentrations of BaP during early development. Tocofersolan shows antioxidant activity. Tocofersolan can be used to provide an orally bioavailable source of vitamin E .
    Tocofersolan
  • HY-B1849
    Hexazinone

    		Environmental Pollutants Herbicide Others
    Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .
    Hexazinone
  • HY-150080
    GSK3739936

    BMS-986180

    		 HIV HIV Integrase Infection
    GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
    GSK3739936
  • HY-B1849R
    Hexazinone (Standard)

    		Reference Standards Environmental Pollutants Herbicide Others
    Hexazinone (Standard) is the analytical standard of Hexazinone. This product is intended for research and analytical applications. Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .
    Hexazinone (Standard)
  • HY-147654
    PROTAC Hemagglutinin Degrader-1

    		PROTACs Influenza Virus Infection
    PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity .
    PROTAC Hemagglutinin Degrader-1
  • HY-B1849S
    Hexazinone-d6

    		Isotope-Labeled Compounds Environmental Pollutants Herbicide Others
    Hexazinone-d6 is the deuterium labeled Hexazinone. Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .
    Hexazinone-d6
  • HY-171292
    CK1δ-IN-9

    		Casein Kinase p38 MAPK Others
    CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC50 of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC50 of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance .
    CK1δ-IN-9
  • HY-115004
    MM-433593

    		FAAH Neurological Disease
    MM-433593 is a potent and selective inhibitor of fatty acid amide hydrolase-1 (FAAH-1) that is orally administered to inhibit pain, inflammation, and related disorders. Pharmacokinetic studies of MM-433593 in macaques revealed a biphasic elimination profile with a rapid distribution phase and a slower elimination phase, with a systemic clearance of 8-11 mL/min/kg. MM-433593 exhibits moderate oral bioavailability (14-21%) and its metabolism primarily involves oxidation of the methyl group on the indole ring, resulting in a variety of sulfate, glucuronide, or glutathione-conjugated metabolites .
    MM-433593
  • HY-120184
    VU0467485

    AZ13713945

    		 mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
    VU0467485
  • HY-166594S
    Deucravacitinib-13C,d3

    		Isotope-Labeled Compounds IFNAR Interleukin Related JAK Inflammation/Immunology
    Deucravacitinib- 13C,d3 is the 13C- and deuterium labeled Deucravacitinib. Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .
    Deucravacitinib-13C,d3
  • HY-183335
    SMO-IN-6

    		Smo Hedgehog Gli Apoptosis Caspase Cancer
    Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma .
    SMO-IN-6
  • HY-16265A
    JI-101 hydrochloride

    		Ephrin Receptor PDGFR VEGFR Cancer
    JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
    JI-101 hydrochloride

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