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human Caco-2 cell monolayers

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-168046
    ALG-055009

    		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-148447
    eIF4A-IN-3

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A-IN-3, Silvestrol (HY-13251) analogue, is an eIF4A inhibitor. eIF4A-IN-3 blocks protein translation initiation by interfering with eIF4F complex assembly, preferentially inhibiting translation of mRNAs with long, highly structured 5'-untranslated regions. eIF4A-IN-3 inhibits proliferation of human breast cancer cells. eIF4A-IN-3 has moderate apical to basolateral permeability in intestinal cell monolayers and a low efflux ratio .
    eIF4A-IN-3
  • HY-W099633
    2-Aminodecanoic acid

    		Amino Acid Derivatives Neurological Disease
    2-Aminodecanoic acid is a lipophilic α-amino acid with an aliphatic side chain of 10 carbon atoms. 2-Aminodecanoic acid modifies the N-terminus of endogenous opioid peptide endomorphin-1 to enhance metabolic stability and membrane permeability. 2-Aminodecanoic acid can be used for the research of neuropathic pain .
    2-Aminodecanoic acid
  • 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
  • HY-14296A
    PF-610355 (hydrochloride)

    		Adrenergic Receptor Inflammation/Immunology
    PF-610355 hydrochloride is a β2-adrenergic receptor (β2-AR) full agonist with selectivity for β1-adrenergic receptors. PF-610355 hydrochloride increases intracellular cAMP levels, induces sustained tracheal smooth muscle relaxation, and inhibits acetylcholine-induced bronchoconstriction. PF-610355 hydrochloride can be used in research related to chronic obstructive pulmonary disease, asthma, and respiratory system diseases .
    PF-610355 (hydrochloride)
  • HY-182421
    GPR54 antagonist-1

    		Kisspeptin Receptor Endocrinology Cancer
    GPR54 antagonist‑1 is a GPR54 antagonist with IC50 values of 3.6 nM and 15 nM against human and rat GPR54, respectively. GPR54 antagonist‑1 shows blood‑brain barrier penetration. GPR54 antagonist‑1 blocks the function of human and rat GPR54 receptors. GPR54 antagonist‑1 suppresses plasma luteinizing hormone levels in castrated male rats. GPR54 antagonist‑1 can be used for the study of prostate cancer and endometriosis .
    GPR54 antagonist-1
  • HY-186072
    NT-0527

    		NOD-like Receptor (NLR) Interleukin Related Cytochrome P450 Neurological Disease Metabolic Disease Inflammation/Immunology
    NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
    NT-0527

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