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ASP3662

Chemical Structure : ASP3662

CAS No.: 1204178-50-6

ASP3662 (Clofutriben, ASP 3662, ASP-3662)

Catalog No.: PC-35375Not For Human Use, Lab Use Only.

ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

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    Biological Activity

    ASP3662 (Clofutriben) is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.
    ASP3662 (Clofutriben) demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.)。
    ASP3662 (Clofutriben) inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord。
    ASP3662 (Clofutriben) ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats.

    Physicochemical Properties

    M.Wt 424.808
    Formula C19H16ClF3N4O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-{5-[2-(4-chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide

    References

    1. Kiso T, et al. Br J Pharmacol. 2018 Jul 14. doi: 10.1111/bph.14448.

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