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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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| AZ-4217
AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. |
| Se-Methylselenocysteine hydrochloride
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. |
| Glabrolide
Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor. |
| Kushenol C
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM. |
| Deoxyneocryptotanshinone
Deoxyneocryptotanshinone is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. |
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