gamma-secretase modulator 5

Modify Date: 2024-01-12 09:44:39

gamma-secretase modulator 5 Structure
gamma-secretase modulator 5 structure
Common Name gamma-secretase modulator 5
CAS Number 1353570-53-2 Molecular Weight 435.55
Density N/A Boiling Point N/A
Molecular Formula C22H25N7OS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of gamma-secretase modulator 5


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].

 Names

Name gamma-secretase modulator 5

 gamma-secretase modulator 5 Biological Activity

Description 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].
Related Catalog
Target

Aβ38:305 nM (EC50)

Aβ40:104 nM (IC50)

Aβ42:60 nM (IC50)

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].
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
References

[1]. Kevin D Rynearson, et al. Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators. Bioorg Med Chem. 2020 Nov 15;28(22):115734.

 Chemical & Physical Properties

Molecular Formula C22H25N7OS
Molecular Weight 435.55