Beta-secretase Inhibitor IV is a potent cell-penetrating inhibitor that binds to the active site of BACE-1 and blocks its proteolytic activity (IC50 = 15 nM for BACE-1, human and 29 nM for HEK293-APPNFEV cells sAPP_NF). The IC50 of BACE-2, cathepsin D and renin were 230 nM, 7.6 μM and >50 μM, respectively.
| Molecular Weight | 578.72 |
| Formula | C31H38N4O5S |
| CAS Number | 797035-11-1 |
| Solubility (25°C) | DMSO: 100 mg/mL |
| Storage | 2-8℃, protect from light, dry, sealed |
| 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] Ramn Cacabelos, et al. CNS Neurol Disord Drug Targets. Novel Therapeutic Strategies for Dementia
[4] Giuseppe Grasso. Mass Spectrom Rev. The use of mass spectrometry to study amyloid-β peptides
| 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. |
| Aloenin
Aloenin (Aloenin A) is a natural compound, which has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE). |
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