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Submit ReviewLY 2886721 Hydrochloride
Description: Potent and selective β-secretase (BACE) inhibitor
Chemical Name: N-[3-[(4aS,7aS)-2-Amino-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for LY 2886721 Hydrochloride
LY 2886721 Hydrochloride is a potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.
Compound Libraries for LY 2886721 Hydrochloride
LY 2886721 Hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LY 2886721 Hydrochloride
| M. Wt | 426.87 |
| Formula | C18H16F2N4O2S.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1262036-49-6 |
| PubChem ID | 50902942 |
| InChI Key | JHHMCINLHBUFHB-GHDSXOKHSA-N |
| Smiles | [H][C@@]12COC[C@]1(C3=CC(NC(C4=CC=C(C=N4)F)=O)=CC=C3F)N=C(SC2)N.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LY 2886721 Hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.69 | 100 |
Preparing Stock Solutions for LY 2886721 Hydrochloride
The following data is based on the product molecular weight 426.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.34 mL | 11.71 mL | 23.43 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.69 mL |
| 10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets for LY 2886721 Hydrochloride
References for LY 2886721 Hydrochloride
References are publications that support the biological activity of the product.
May et al (2015) The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs and humans. J.Neurosci. 35 1199 PMID: 25609634
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