ASP3662

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ASP3662 是一种有效、选择性、CNS 渗透性、口服活性的 11β-HSD1 抑制剂，对人、小鼠和大鼠 11β-HSD1 的 Ki 分别为 5.3、2.6 和 23 nM。

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; demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.); inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord; ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats.Alzheimer Disease Phase 2 Discontinued.

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ASP 3662 | ASP-3662

Metabolic Enzyme/Protease

11β-HSD

11β-HSD

Neurological Disease

Alzheimer Disease

1204178-50-6

424.808

C19H16ClF3N4O2

>98% (HPLC)

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CC(C)(C1=NN=C(N1C)C2=C(C=C(C=C2)C(=O)N)F)OC3=C(C=C(C=C3F)Cl)F

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

(-20℃)

With Ice Pack

≥ 2 years