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.
| Molecular Weight | 390.41 |
| Formula | C18H16F2N4O2S |
| CAS Number | 1262036-50-9 |
| Solubility (25°C) | DMSO |
| 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.
[3] Alvaro Miranda, et al. Selective Secretase Targeting for Alzheimer's Disease Therapy
| Related BACE Products |
|---|
| 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. |
| β-Secretase Inhibitor IV
β-Secretase Inhibitor IV is a cellular permeability inhibitor that binds to the active site of BACE-1 and blocks its proteolytic activity (IC₅₀= 15 nM in human BACE-1). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
