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PF-06751979
PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).
Catalog No. T12429Cas No. 1818339-66-0
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PF-06751979
Catalog No. T12429Cas No. 1818339-66-0
PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,230 | 10-14 weeks | |
| 50 mg | $1,610 | 10-14 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 | BACE2:194 nM , BACE1:7.3 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 |
Storage & Solubility Information
| 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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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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