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.
| Molecular Weight | 409.41 |
| Formula | C17H17F2N5O3S |
| CAS Number | 1286770-55-5 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[2] Matthew E Kennedy, et al. Verubecestat for Prodromal Alzheimer's Disease. Reply
[3] Shaomin Li, et al. Verubecestat for Prodromal Alzheimer's Disease
[4] Michael F Egan, et al. Randomized Trial of Verubecestat for Prodromal Alzheimer's Disease
[5] Michael F Egan, et al. Randomized Trial of Verubecestat for Mild-to-Moderate Alzheimer's Disease
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