An inhibitor of γ-secretase
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PF-3084014

Item No. 27061

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-N-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1H-imidazol-4-yl]-pentanamide
CAS Number
1290543-63-3
Molecular Formula
C27H41F2N5O
Formula Weight
489.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
FC1=CC(F)=C2C(CC[C@H](N[C@@H](CCC)C(NC3=CN(C(C)(C)CNCC(C)(C)C)C=N3)=O)C2)=C1
InChi Code
InChI=1S/C27H41F2N5O/c1-7-8-23(32-20-10-9-18-11-19(28)12-22(29)21(18)13-20)25(35)33-24-14-34(17-31-24)27(5,6)16-30-15-26(2,3)4/h11-12,14,17,20,23,30,32H,7-10,13,15-16H2,1-6H3,(H,33,35)/t20-,23-/m0/s1
InChi Key
VFCRKLWBYMDAED-REWPJTCUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $219

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    25 mg

    $462

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    Product Description

    PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).1 It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lanz, T.A., Wood, K.M., Richter, K.E.G., et al. Pharmacodynamics and pharmacokinetics of the γ-secretase inhibitor PF-3084014. J. Pharmacol. Exp. Ther. 334(1), 269-277 (2010).