LY2886721 is an orally-available, furothiazine-based inhibitor of b-amyloid protein cleaving enzyme (BACE) for the treatment of Alzheimer's disease. [1] It inhibits recombinant hBACE1 with an IC50 of 20 nM. [2] In cellular assays, LY2886721 inhibits Abeta with an IC50 range of 10-19 nM. Oral administration of LY2886721 to PDAPP mice produced dose-dependent reductions in brain Abeta, C99, and sAPPbeta. [2]
Technical information:
Chemical Formula: | C18H16F2N4O2S | |
CAS #: | 1262036-50-9 | |
Molecular Weight: | 390.41 | |
Purity: | > 98% | |
Appearance: | White | |
Chemical Name: | N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide | |
Solubility: | Up to 20 mM in DMSO | |
Synonyms: | LY-2886721, LY 2886721, LY2886721 |
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. | Alzheimer's Disease Research Unit Studies synopsis (April 1, 2012) |
2. | Alzheimer Assocation International Conference, 2012, Oral Sessions (O1-06-03): "Preclinical Characterization of LY2886721: A BACE1 inhibitor in clinical developmetn for early Alzheimer's disease" |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.