A γ-secretase inhibitor
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BMS-299897

Item No. 35777

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(1R)-1-[[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoro-benzenebutanoic acid
CAS Number
290315-45-6
Molecular Formula
C24H21ClF3NO4S
Formula Weight
511.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Methanol: soluble
SMILES
C[C@H](C1=C(C=C(C=C1)F)CCCC(O)=O)N(C2=C(C=CC(F)=C2)F)S(=O)(C3=CC=C(C=C3)Cl)=O
InChi Code
InChI=1S/C24H21ClF3NO4S/c1-15(21-11-7-18(26)13-16(21)3-2-4-24(30)31)29(23-14-19(27)8-12-22(23)28)34(32,33)20-9-5-17(25)6-10-20/h5-15H,2-4H2,1H3,(H,30,31)/t15-/m1/s1
InChi Key
IZAOBRWCUGOKNH-OAHLLOKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $125

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    10 mg

    $186

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    25 mg

    $310

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    Product Description

    BMS-299897 is an inhibitor of γ-secretase.1,2,3 It selectively cleaves the carboxy terminal fragment (CTF) of amyloid precursor protein (APP) over the Notch-1 CTF in HEK293 cells (IC50s = 7.1 and 105.9 nM, respectively).2 BMS-299897 (0.1-1 nmol/animal) reduces increases in amyloid-β (1-42) (Aβ42) levels induced by Aβ (25-35) in the mouse hippocampus.3 It also prevents deficits induced by Aβ (25-35) in the novel object recognition test when tested with a one-hour, but not a 24-hour, intertrial interval in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tian, G., Sobotka-Briner, C.D., Zysk, J., et al. Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines. The Journal of Biological Chemisty 277(35), 31499-31505 (2002).

    2. Barten, D.M., Guss, V.L., Corsa, J.A., et al. Dynamics of β-amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor. J. Pharmacol. Exp. Ther. 312(2), 635-643 (2005).

    3. Meunier, J., Villard, V., Givalois, L., et al. The γ-secretase inhibitor 2-[(1R)-1-[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl) amino]ethyl-5-fluorobenzenebutanoic acid (BMS-299897) alleviates Aβ1-42 seeding and short-term memory deficits in the Aβ25-35 mouse model of Alzheimer’s disease. Eur. J. Pharmacol. 698(1-3), 193-199 (2013).