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Verubecestat (MK-8931)

Cat. No. M9386
Verubecestat (MK-8931) Structure
Synonym:

MK-8931

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Biological Activity

Verubecestat (MK-8931) is a BACE1 inhibitor with Ki values of 2.2 and 3.4 nM for human and mouse Bace1, respectively. Verubecestat could also inhibit the production of Ab40, Ab42, and sAPPb in human cells with similar potency.

In vivo, treatment of rats and monkeys with verubecestat at exposures >40-fold higher than those tested in clinical trials did not cause many of the adverse effects previously reported to BACE inhibition.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 409.41
Formula C17H17F2N5O3S
CAS Number 1286770-55-5
Purity >98%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Verubecestat (MK-8931), MK-8931 supplier, BACE, inhibitors

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