1. Neuronal Signaling
  2. Amyloid-β
  3. gamma-secretase modulator 5

gamma-secretase modulator 5 (compound 22d) 是一种可以通过血脑屏障的 γ-分泌酶调节剂 (GSMs),可以抑制聚集的淀粉样蛋白 β 肽 Aβ42 的产生,其 IC50 值为 60 nM。可以用于阿尔茨海默病的研究。

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gamma-secretase modulator 5 Chemical Structure

gamma-secretase modulator 5 Chemical Structure

CAS No. : 1353570-53-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

gamma-secretase modulator 5 (compound 22d) is a brain-penetrant gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease[1].

IC50 & Target[1]

Aβ38

305 nM (EC50)

Aβ40

104 nM (IC50)

Aβ42

60 nM (IC50)

体外研究
(In Vitro)

gamma-secretase modulator 5 (compound 22d) (1-10 μM, 24 h) does not affect the function of the APP751 enzyme and not inhibit Notching processing in H4 human neuroglioma cells over-expressing human APP751[1].
gamma-secretase modulator 5 (compound 22d) acts on Aβ38 with the EC50 value of 305 nM and acts on Aβ40 with the IC50 value of 104 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The pharmacokinetic parameters of gamma-secretase modulator 5 (compound 22d) in male CD-1 mice[1].

Parameters IV PO
Dose (mg/kg) 1 5
Cmax (ng/mL) 824 705
Tmax (h) 0.083 0.25
t1/2 (h) 0.5 -
AUClast (ng•h/mL) 443 1089
AUCinf (ng•h/mL) 463 1243
Cl (mL/h/kg) 2159 -
Vss (mL/kg) 1413 -
F (%) 100 53.7

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

435.55

Formula

C22H25N7OS

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

gamma-secretase modulator 5 相关分类

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gamma-secretase modulator 5
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