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。
产品描述
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 IC 50 value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease [1].
体外活性
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 EC 50 value of 305 nM and acts on Aβ40 with the IC 50 value of 104 nM [1].
体内活性
The pharmacokinetic parameters of gamma-secretase modulator 5 (compound 22d) in male CD-1 mice [1]. Parameters IV PO Dose (mg/kg) 1 5 C max (ng/mL) 824 705 T max (h) 0.083 0.25 t 1/2 (h) 0.5 - AUC last (ng h/mL) 443 1089 AUC inf (ng h/mL) 463 1243 Cl (mL/h/kg) 2159 - Vss (mL/kg) 1413 - F (%) 100 53.7
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years