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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-11β-HSD-ASP3662
ASP3662

Chemical Structure : ASP3662

CAS No.: 1204178-50-6

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ASP3662 (Clofutriben, ASP 3662, ASP-3662)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 424.808
    分子式 C19H16ClF3N4O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

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

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