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Biochem/physiol Actions
Brain-penetrant, orally active, highly potent and selective gamma-secretase inhibitor with CNS Aβ40-lowering efficacy in mice and rats in vivo.
MRK-560 is a brain-penetrant, orally active, highly potent and selective gamma-secretase inhibitor (GSI; IC50 = 0.65 nM by SH-SY5Y cellular γ-secretase substrate A4CTF breakdown assay) with little inhibitory potency against a panel of 171 enzymes/receptors. MRK-560 blocks Aβ40 & Aβ42 production with similar potency in SH-SY5Y cultures (IC50 <0.5 nM) and lowers CNS Aβ40 in rats (brain & SCF ED50 in 8h = 6 & 10 mg/kg po.) and APP-YAC mice (brain ED50 in 4h <3 mg/kg po.) in vivo
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | FC(F)(F)[S](=O)(=O)N[C@@H]1CC[C@@](CC1)([S](=O)(=O)c3ccc(cc3)Cl)c2c(ccc(c2)F)F |
| 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 |
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¥ 1596.77
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