MedKoo Cat#: 562016 | Name: PF-06648671
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PF-06648671 is a γ-secretase modulator or Amyloid precursor protein secretase modulator for the treatment of neurodegenerative and/or neurological disorders such as Alzheimer’s disease and Down’s Syndrome. PF-06648671 decreased Aβ42 and Aβ40 concentrations in CSF, with greater effects on Aβ42, and increased Aβ37 and Aβ38 levels, particularly Aβ37. No significant change in total Aβ was observed. PF-06648671 resulted in robust, dose-dependent reductions in CSF Aβ42 and Aβ40 and elevations in Aβ37 and Aβ38, with no effect on total Aβ.

Chemical Structure

PF-06648671
PF-06648671
CAS#1587727-31-8

Theoretical Analysis

MedKoo Cat#: 562016

Name: PF-06648671

CAS#: 1587727-31-8

Chemical Formula: C25H23ClF4N4O3

Exact Mass: 538.1395

Molecular Weight: 538.93

Elemental Analysis: C, 55.72; H, 4.30; Cl, 6.58; F, 14.10; N, 10.40; O, 8.91

Price and Availability

Size Price Availability Quantity
1mg USD 90.00 Ready to Ship
5mg USD 250.00 Ready to Ship
10mg USD 450.00 Ready to Ship
25mg USD 850.00 Ready to Ship
50mg USD 1,350.00 Ready to Ship
100mg USD 2,350.00 Ready to Ship
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Related CAS #
No Data
Synonym
PF-06648671; PF 06648671; PF06648671; PF-6648671; PF 6648671; PF6648671;
IUPAC/Chemical Name
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
InChi Key
AKCDDYGYIGPEKL-JQOQJDEVSA-N
InChi Code
InChI=1S/C25H23ClF4N4O3/c1-13-11-32(12-31-13)19-3-4-20-24(36)33(7-8-34(20)23(19)35)14(2)21-5-6-22(37-21)15-9-18(27)17(26)10-16(15)25(28,29)30/h3-4,9-12,14,21-22H,5-8H2,1-2H3/t14-,21-,22+/m0/s1
SMILES Code
O=C1C(N2CCN1[C@H]([C@H]3O[C@@H](C4=CC(F)=C(Cl)C=C4C(F)(F)F)CC3)C)=CC=C(N5C=C(C)N=C5)C2=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM).
In vitro activity:
TBD
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 538.93 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
Ahn JE, Carrieri C, Dela Cruz F, Fullerton T, Hajos-Korcsok E, He P, Kantaridis C, Leurent C, Liu R, Mancuso J, Mendes da Costa L, Qiu R. 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. doi: 10.1002/cpt.1570. Epub 2019 Sep 11. PMID: 31314925; PMCID: PMC6977340. Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Butler TW, Dorff PH, Efremov IV, Evrard E, Green ME, Helal CJ, Kauffman GW, Mullins PB, Navaratnam T, O'Donnell CJ, O'Sullivan TJ, Patel NC, Stepan AF, Stiff CM, Subramanyam C, Trapa P, Tran TP, Vetelino BC, Yang E, Xie L, Pustilnik LR, Steyn SJ, Wood KM, Bales KR, Hajos-Korcsok E, Verhoest PR. Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease. J Med Chem. 2024 Jun 27;67(12):10248-10262. doi: 10.1021/acs.jmedchem.4c00580. Epub 2024 Jun 7. PMID: 38848667.