A potent inhibitor of γ-secretase
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MRK-560

Item No. 27599

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoro-methanesulfonamide
CAS Number
677772-84-8
Molecular Formula
C19H17ClF5NO4S2
Formula Weight
517.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 50 mM
SMILES
O=S(N[C@H]1CC[C@](S(C2=CC=C(Cl)C=C2)(=O)=O)(C3=C(F)C=CC(F)=C3)CC1)(C(F)(F)F)=O
InChi Code
InChI=1S/C19H17ClF5NO4S2/c20-12-1-4-15(5-2-12)31(27,28)18(16-11-13(21)3-6-17(16)22)9-7-14(8-10-18)26-32(29,30)19(23,24)25/h1-6,11,14,26H,7-10H2/t14-,18+
InChi Key
WDZVWDXOIGQJIO-UJKQEGAGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $117

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    5 mg

    $400

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    Product Description

    MRK-560 is a potent inhibitor of γ-secretase (IC50 = 0.65 nM).1 In vivo, MRK-560 (1-10 mg/kg) reduces diethanolamine-soluble amyloid-β (1-40) (Aβ40) levels in APP-YAC transgenic mouse brain. MRK-560 reduces brain and cerebrospinal fluid Aβ40 levels in rats (ED50s = 6 and 10 mg/kg, respectively).2 It also decreases brain-soluble Aβ40 and Aβ42 levels and recovers hippocampal long-term potentiation in the Tg2576 transgenic mouse model of Alzheimer's disease.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Churcher, I., Beher, D., Best, J.D., et al. 4-Substituted cyclohexyl sulfones as potent, orally active γ-secretase inhibitors. Bioorg. Med. Chem. Lett. 16(2), 280-284 (2006).

    2. Best, J.D., Jay, M.T., Otu, F., et al. In vivo characterization of Aβ(40) changes in brain and cerebrospinal fluid using the novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. J. Pharmacol. Exp. Ther. 317(2), 786-790 (2006).

    3. Townsend, M., Qu, Y., Gray, A., et al. Oral treatment with a γ-secretase inhibitor improves long-term potentiation in a mouse model of Alzheimer’s disease. J. Pharmacol. Exp. Ther. 333(1), 110-119 (2010).