δ-secretase inhibitor 11

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

δ-分泌酶抑制剂 11 是一种 δ-分泌酶抑制剂，可用作 AD 治疗转化开发的先导化合物。

δ-secretase inhibitor 11 is an inhibitor of δ-secretase and can be used as a lead compound for translational development of AD treatment. (In Vitro):The inhibitory effect of δ-secretase inhibitor 11 on AEP activity in vitro was tested and the dose-response relationship revealed that the δ-secretase inhibitor 11 had an IC50 value of 0.15?±?0.09?μM . (In Vivo):It was found that oral administration of δ-secretase inhibitor 11 (10?mg/kg) significantly suppressed brain AEP activity compared to the vehicle treatment. The concentrations of Aβ1–40 and Aβ1–42 in brain lysates of SAMP8 mice were significantly reduced due to AEP inhibition by δ-secretase inhibitor 11.

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Animal Model:Tau P301S transgenic mice (n=4 mice per group)Dosage:10 mg/kg Administration:Orally, once daily for 3 months Result:Significantly inhibited the activity of δ-secretase in both wild-type and tau P301S mice brain, increased PP2A activity, and attenuated the truncation and phosphorylation of tau in tau P301S mice. Ameliorated synaptic loss and restored synaptic dysfunction in tau P301S mice.Animal Model:5XFAD mice Dosage:2, 5 or 10?mg?kg Administration:Orally, once daily for 1.5 and 3 months Result:Attenuated the β-secretase-mediated processing of APP, significantly decreased the concentrations of Aβ 1-40 and Aβ 1-42 in the brain lysates, and attenuated Aβ deposition in a time- and dose-dependent manner.

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Membrane Transporter/Ion Channel

Beta Amyloid

COX-2

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842964-18-5

220.232

C10H12N4O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (567.59 mM)

Nc1ccc(N2CCOCC2)c2nonc12

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(-20℃)

With Ice Pack

≥ 2 years