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Verubecestat

Chemical Structure : Verubecestat

CAS No.: 1286770-55-5

Verubecestat (MK-8931, MK8931)

Catalog No.: PC-45073Not For Human Use, Lab Use Only.

Verubecestat (MK-8931) is a potent, selective, structurally unique BACE inhibitor with Ki of 2.2 nM and 0.38 nM for BACE1 and BACE2, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Verubecestat (MK-8931) is a potent, selective, structurally unique BACE inhibitor with Ki of 2.2 nM and 0.38 nM for BACE1 and BACE2, respectively.
Verubecestat (MK-8931) displays high selectivity for BACE1 over other key aspartyl proteases, notably cathepsin D.
Verubecestat (MK-8931) reduces plasma, cerebrospinal fluid (CSF), and brain concentrations of Aβ40, Aβ42, and sAPPβ.
Verubecestat (MK-8931) is well tolerated and produces reductions in Aβ40, Aβ42, and sAPPβ in the CSF of both healthy human subjects and AD patients in clinical evaluation.

Physicochemical Properties

M.Wt 409.4104
Formula C17H17F2N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 35 mg/mL

Chemical Name/SMILES

2-Pyridinecarboxamide, N-[3-[(5R)-3-amino-5,6-dihydro-2,5-dimethyl-1,1-dioxido-2H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-fluoro-

References

1. Kennedy ME,, et al. Sci Transl Med. 2016 Nov 2;8(363):363ra150.

2. Scott JD, et al. J Med Chem. 2016 Dec 8;59(23):10435-10450.

3. Villarreal S, et al. J Alzheimers Dis. 2017;59(4):1393-1413.

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