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PF-06648671 

Cat. No. M28634
PF-06648671  Structure
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Biological Activity

PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.

Chemical Information
Molecular Weight 538.92
Formula C25H23ClF4N4O3
CAS Number 1587727-31-8
Form Solid
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jae Eun Ahn, et al. Clin Pharmacol Ther. Pharmacokinetic and Pharmacodynamic Effects of a γ-Secretase Modulator, PF-06648671, on CSF Amyloid-β Peptides in Randomized Phase I Studies

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06648671  supplier, Gamma-secretase/Beta-secretase, inhibitors, activators


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