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| | 2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione Basic information |
| Product Name: | 2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione | | Synonyms: | PF-06648671;2H-Pyrido[1,2-a]pyrazine-1,6-dione, 2-[(1S)-1-[(2S,5R)-5-[4-chloro-5-fluoro-2-(trifluoromethyl)phenyl]tetrahydro-2-furanyl]ethyl]-3,4-dihydro-7-(4-methyl-1H-imidazol-1-yl)-;PF 6648671;PF6648671;PF-6648671;2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione , PF-06648671;Propofol Impurity 33;2-[(1S)-1-[(2S,5R)-5-[4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl]tetrahydro-2-furanyl]ethyl]-3,4-dihydro-7-(4-methyl-1H-imidazol-1- yl)-2H-pyrido[1,2-a]pyrazine-1,6-dione | | CAS: | 1587727-31-8 | | MF: | C25H23ClF4N4O3 | | MW: | 538.92 | | EINECS: | | | Product Categories: | | | Mol File: | 1587727-31-8.mol | ![2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione Structure](CAS/20200119/GIF/1587727-31-8.gif) |
| | 2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml | | form | Solid | | color | White to off-white |
| | 2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione Usage And Synthesis |
| Uses | 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[1]. | | 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[1].
In a cell‐based assay, PF‐06648671 reduces Aβ42 and Aβ40 , with concomitant increases in Aβ37 and Aβ38, without inhibiting the cleavage of Notch or other substrates[1].
PF‐06648671 demonstrates reduces Aβ42 within the brain and CSF following acute oral administration in animals[1]. | | in vivo | PF-06648671 demonstrates reduces Aβ42 within the brain and CSF following acute oral administration in animals[1]. | | References | [1] Jae Eun Ahn, et al. Pharmacokinetic and Pharmacodynamic Effects of a γ-Secretase Modulator, PF-06648671, on CSF Amyloid-β Peptides in Randomized Phase I Studies. Clin Pharmacol Ther 2020 Jan;107(1):211-220.
[2] MARTIN PETTERSSON*, PATRICK R. VERHOEST Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer’s Disease[J]. Journal of Medicinal Chemistry, 2024, 67 12: 10248-10262. DOI: 10.1021/acs.jmedchem.4c00580 |
| | 2-((S)-1-((2S,5R)-5-(4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl)tetrahydrofuran-2-yl)ethyl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione Preparation Products And Raw materials |
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