LY-2811376 is a orally-available, non-peptidic inhibitor of hBACE1 with an IC50 of 239 nM. Selectivity of LY-2811376 for BACE1 over BACE2 was found to be 10-fold, and 50-fold or greater over related aspartyl proteases cathepsin D, pepsin, or renin. [1] In APP-overexpressing human embryonic kidney cell lines, LY-2811376 treatment decreased Ab secretion in a concentration-dependent fashion, with an EC50 of ~300 nM. In primary neuronal cultures of PDAPP transgenic mouse, Ab secretion was measured at an EC50 of ~100 nM.
In vivo, LY2811376 inhibits BACE1 activity by concomitantly reducing C99 and sAPPb, the two primary APP cleavage products generated by BACE1.
Technical information:
| Chemical Formula: | C15H14F2N4S | |
| CAS #: | 1194044-20-6 | |
| Molecular Weight: | 320.36 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | (S)-4-(2,4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine | |
| Solubility: | Up to 50 mM in DMSO | |
| Synonyms: | LY-2811376, LY 2811376, LY2811376 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | May et al., Robust central reduction of amyloid-? in humans with an orally available, non-peptidic ?-secretase inhibitor. J. Neurosci., 2011, 31(46), 16507-16516. Pubmed ID: 22090477 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
