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LY2811376

Cat. No. M2172
LY2811376 Structure
Size Price Availability Quantity
2mg USD 64  USD64 In stock
5mg USD 120  USD120 In stock
10mg USD 230  USD230 In stock
50mg USD 690  USD690 In stock
100mg USD 900  USD900 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 320.36
Formula C15H14F2N4S
CAS Number 1194044-20-6
Solubility (25°C) Ethanol 48 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Lachno DR, et al. J Alzheimers Dis. 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.

[2] May PC, et al. J Neurosci. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.

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  Catalog
Abmole Inhibitor Catalog




Keywords: LY2811376 supplier, Gamma-secretase/Beta-secretase, inhibitors, activators


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