A γ-secretase modulator
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PF-06648671

Item No. 41893

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
1587727-31-8
Synonyms
  • GSM22
Molecular Formula
C25H23ClF4N4O3
Formula Weight
538.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@H](N1C(C(N2CC1)=CC=C(N3C=NC(C)=C3)C2=O)=O)[C@@]4([H])O[C@@H](C5=CC(F)=C(Cl)C=C5C(F)(F)F)CC4
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
InChi Key
AKCDDYGYIGPEKL-JQOQJDEVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $138

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    1 mg

    $248

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    5 mg

    $963

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    10 mg

    $1,100

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    Product Description

    PF-06648671 is a γ-secretase modulator.1 It selectively inhibits the production of amyloid-β (1-42) (Aβ42) in CHO cells expressing wild-type amyloid precursor protein (APP; IC50 = 9.8 nM) over Notch cleavage to its signaling effector Notch intracellular domain (NICD; IC50 = >15.8 µM). PF-06648671 (10 and 40 mg/kg) decreases brain levels of Aβ42 in rats. It also decreases cerebrospinal fluid (CSF) levels of Aβ40 and Aβ42 and increases levels of Aβ38 and Aβ39, without affecting total Aβ CSF levels, in dogs when administered at a dose of 20 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pettersson, M., Johnson, D.S., Humphrey, J.M., et al. Discovery of clinical candidate PF-06648671: A potent γ-secretase modulator for the treatment of Alzheimer’s disease. J. Med. Chem. 67(12), 10248-10262 (2024).