产品
编 号：F744313
分子式：C22H25N7OS
分子量：435.55
分子式：C22H25N7OS
分子量：435.55
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CAS No: 1353570-53-2
产品详情
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.
体内研究：
The pharmacokinetic parameters of gamma-secretase modulator 5 (compound 22d) in male CD-1 mice.ParametersIVPO
Dose (mg/kg)15
Cmax (ng/mL)824705
Tmax (h)0.0830.25
t1/2 (h)0.5-
AUClast (ng?h/mL)4431089
AUCinf (ng?h/mL)4631243
Cl (mL/h/kg)2159-
Vss (mL/kg)1413-
F (%)10053.7
体外研究：
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.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.
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.
体内研究：
The pharmacokinetic parameters of gamma-secretase modulator 5 (compound 22d) in male CD-1 mice.ParametersIVPO
Dose (mg/kg)15
Cmax (ng/mL)824705
Tmax (h)0.0830.25
t1/2 (h)0.5-
AUClast (ng?h/mL)4431089
AUCinf (ng?h/mL)4631243
Cl (mL/h/kg)2159-
Vss (mL/kg)1413-
F (%)10053.7
体外研究：
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.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.
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