Verubecestat

Key Product Details

Product Description

Verubecestat is a high affinity and selective β-secretase 1 (BACE1) and its homolog BACE2 inhibitor (K_i of 2.2 nM and 0.38 nM respectively). It exhibits no inhibition of cathepsin D, cathepsin E, pepsin, or renin. Verubecestat potently reduces Aβ40 formation in HEK293 APP^Swe/Lon cells (IC₅₀ = 2.1 nM). Verubecestat significantly lowers CSF and brain Aβ levels in rats. Orally bioavailable.

Product Specifications for Verubecestat

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Verubecestat

The following data is based on the product molecular weight 409.41.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.44 mL	12.21 mL	24.43 mL
5 mM	0.49 mL	2.44 mL	4.89 mL
10 mM	0.24 mL	1.22 mL	2.44 mL
50 mM	0.05 mL	0.24 mL	0.49 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Scott Discovery of the 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative Verubecestat (MK-8931) - A β-site amyloid precursor protein cleaving enzyme 1 inhibitor for the treatment of Alzheimer's disease. J.Med.Chem. 2016 PMID: 27933948

Product Documents for Verubecestat