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PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,230 | 10-14 weeks | |
50 mg | $1,610 | 10-14 weeks |
Description | PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay). |
Targets&IC50 | BACE1:7.3 nM , BACE2:194 nM |
In vitro | PF-06751979 demonstrates enhanced selectivity for BACE2 (IC50=194 nM) with a 27-fold improvement compared to literature examples and various chemical series in the BACE1 program. |
In vivo | PF-06751979 demonstrates excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases, including BACE2. Acute administration results in a robust, dose-responsive, and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40, with peak inhibition of over 77% at 3 hours. [1]. |
Molecular Weight | 455.5 |
Formula | C18H19F2N5O3S2 |
Cas No. | 1818339-66-0 |
Relative Density. | 1.66 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 50 mg/mL (109.77 mM), Sonication is recommended. DMSO: 150 mg/mL (329.31 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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