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LY2811376

Cat. No. M2172
LY2811376 Structure
Size Price Availability Quantity
10mg USD 260 In stock
50mg USD 800 In stock
100mg USD 1160 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LY2811376 is the first orally available non-peptidic BACE1 inhibitor that produces profound Aβ-lowering effects in animals. LY2811376 has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. LY2811376 inhibits Aβ secretion with EC50 of ~100 nM in primary neuronal cultures of PDAPP transgenic mouse. Administration of LY2811376 (10, 30 and 100 mg/kg doses) results in dose-dependent, significant reductions in Aβ, as well as sAPPβ and C99. LY2811376 treatment yields a concentration-dependent decrease in Aβ secretion in APP-overexpressing HEK293 cells.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 320.36
Formula C15H14F2N4S
CAS Number 1194044-20-6
Purity >99%
Solubility Ethanol 50 mg/mL
Storage at -20°C
References

Validation of a multiplex assay for simultaneous quantification of amyloid-β peptide species in human plasma with utility for measurements in studies of Alzheimer's disease therapeutics.
Lachno DR, et al. J Alzheimers Dis. 2012;32(4):905-18. PMID: 22886018.

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.
May PC, et al. J Neurosci. 2011 Nov 16;31(46):16507-16. PMID: 22090477.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2811376 supplier, Gamma-secretase, inhibitors

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