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high tissue distribution

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10116
    PI-540

    		PI3K mTOR Cancer
    PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM) .
    PI-540
  • HY-137263
    Propionylmaridomycin

    		Antibiotic Infection
    Propionylmaridomycin is a macrolide antibiotic with antibacterial activity. Propionylmaridomycin is rapidly absorbed from the gastrointestinal tract and rapidly distributed to tissues. Propionylmaridomycin radioactivity levels in the liver, kidneys, and lungs were significantly higher than in plasma, while distribution to the brain was less. Propionylmaridomycin is excreted primarily through the feces, and the high fecal recovery rate is due to unabsorbed compounds and biliary excretion of compounds and their metabolites. Propionylmaridomycin exhibits the highest antibacterial activity in the lungs. Propionylmaridomycin is completely converted to several metabolites in rats, of which 4''-depropionyl-9-propionylmaridomycin was identified as the major metabolite .
    Propionylmaridomycin
  • HY-116450
    TISCH

    		Dopamine Receptor Neurological Disease
    TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
    TISCH
  • HY-W205529
    RO 16-6491 free base

    		Fluorescent Dye Neurological Disease
    RO 16-6491 Free base is a selective, reversible inhibitor of monoamine oxidase type B (MAO-B), exhibiting high affinity and specificity for binding sites in human frontal cortex mitochondria and platelet membranes. RO 16-6491 demonstrates a fast dissociation of bound radioactivity at 20 degrees C, indicating its dynamic binding properties. RO 16-6491 also acts as a substrate for MAO-B, suggesting that its oxidation may produce a stable intermediate responsible for its potent inhibitory effects. RO 16-6491 serves as an excellent radioligand probe for investigating the regional tissue distribution of MAO-B in various physiological and pathological states.
    RO 16-6491 free base
  • HY-169059
    Ferroptosis-IN-12

    		Ferroptosis Inflammation/Immunology
    Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
    Ferroptosis-IN-12

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