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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 |
[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
| Related BACE Products |
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| LY2886721
LY2886721 is an effective, selective, orally active inhibitor of beta-site amyloid precursor protein lyase 1 (BACE1) with an IC50 of 20.3 nM against recombinant human BACE1. LY2886721 showed higher selectivity for BACE1 than cathepsin D, pepsin and renin, but lacked selectivity for BACE2 (IC50 was 10.2 nM). LY2886721 crosses the blood-brain barrier and can be used to study Alzheimer's disease. |
| AZD3839
AZD3839 is a potent and selective inhibitor of human BACE1 with Ki of 26.1 nM. |
| Lanabecestat
Lanabecestat (AZD3293, LY3314814) is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor. |
| Eslicarbazepine Acetate
Eslicarbazepine acetate is an antiepileptic drug. |
| LX2343
LX2343 is a BACE1 enzyme inhibitor with IC50 value of 11.43±0.36 μM, and it is a neuroprotective agent. |
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