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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 30 mg/mL|
|Related BACE Products|
The novel once-daily long-acting β2-agonist (LABA) olodaterol is a highly selective and nearly full β2 agonist that provides 24-h bronchodilation in patients with COPD.
AZD3293, also known as LY3314814 is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor.
LY2886721 is an orally-available, furothiazine-based inhibitor of b-amyloid protein cleaving enzyme (BACE).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.