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Purity: ≥98%
LY2886721 (LY 2886721; LY-2886721) is a novel, potent and selective BACE (β-secretase) inhibitor with the potential for the treatment of AD-Alzheimer's Disease. BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid β lowering in nonclinical animal models.
| ln Vitro |
When HEK293Swe cells are exposed to LY2886721 at increasing concentrations over night, the amount of Aβ released into the condition medium decreases in a concentration-dependent manner. The BACE inhibition mechanism is supported by the nearly similar EC50s of 18.5 and 19.7 nM for Aβ1-42 and Aβ1-40 inhibition, respectively[1]. The synthesis of Aβ decreases concentration-dependently when PDAPP neuronal cells are exposed to increasing concentrations of LY2886721 over the course of an overnight exposure. The Aβ1-40 and Aβ1-42 EC50s for inhibition in PDAPP neuronal cultures are similar to those in HEK293Swe cells, with values around 10 nM[1].
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| ln Vivo |
Treatment with LY2886721 (3-30 mg/kg; oral dose; PDAPP mice) dramatically lowers Aβ1-x levels in the cortical and hippocampus regions. Treatment with LY2886721 causes a considerable decrease in C99 and sAPPβ levels in the brain parenchyma[1].
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| Animal Protocol |
Animal/Disease Models: Female hemizygous APPV717F transgenic mice (PDAPP) (2-3 months old)[1]
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: Oral administration Experimental Results: Hippocampal and cortical levels of Aβ1-x were Dramatically decreased . |
| References |
[1]. May PC1, et al. The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. J Neurosci. 2015 Jan 21;35(3):1199-210.
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| Molecular Formula |
C18H16F2N4O2S
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| Molecular Weight |
390.41
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| CAS # |
1262036-50-9
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| Related CAS # |
1262036-49-6
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| SMILES |
FC1=CN=C(C=C1)C(NC2=CC=C(C([C@@]34[C@]([H])(CSC(N)=N4)COC3)=C2)F)=O
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| InChi Key |
NIDRNVHMMDAAIK-YPMLDQLKSA-N
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| InChi Code |
InChI=1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1
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| 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
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5614 mL | 12.8070 mL | 25.6141 mL | |
| 5 mM | 0.5123 mL | 2.5614 mL | 5.1228 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5614 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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