Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Lanabecestat (AZD3293) is a highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor (Ki: 0.4 nM).
Description | Lanabecestat (AZD3293) is a highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor (Ki: 0.4 nM). |
Targets&IC50 | BACE1:0.4 nM (cell free) |
In vitro | Lanabecestat displays a very high target affinity and a markedly slow target off-rate. The off-rate of Lanabecestat has an estimated t1/2 of approximately 9?h. Lanabecestat displays pM potency in primary neuron cultures from mice and guinea pigs and in SH-SY5Y cells over-expressing AβPP (IC50=610 pM, 310 pM, and 80 pM, respectively). |
In vivo | In mice, guinea pigs, and dogs, Lanabecestat displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. |
Cell Research | Cells are incubated with different Lanabecestat concentrations for 5 to 16?h, and the release of sAβPPβ, Aβ1-40, Aβ1-42, or sAβPPα into the medium is analyzed using kits. Cytotoxic effect of Lanabecestat is evaluated in the cell plates using cell proliferation/cytotoxicity kit. |
Animal Research | Female 7- to 14-week-old C57BL/6 mice (n=6 per treatment group and time point) receive a vehicle or Lanabecestat solution at 50, 100, or 200 μmol/kg (20, 41, or 82?mg/kg) as a single dose via oral gavage. Mice and guinea pigs are anesthetized 1.5, 2, 3, 4, 6, 8, 16, 24, or 48?h after the (last) administration of vehicle or drug and are then kept under isoflurane anesthesia. Cerebrospinal fluid (CSF) is aspirated from the cisterna magna, and plasma is isolated from blood collected by cardiac puncture into EDTA tubes. The animals are then sacrificed by decapitation, and the brains are dissected into hemispheres. |
Synonyms | LY3314814, AZD3293 |
Molecular Weight | 412.53 |
Formula | C26H28N4O |
CAS No. | 1383982-64-6 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 100 mg/mL (242.41 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Lanabecestat 1383982-64-6 Neuroscience BACE LY3314814 AZD3293 Inhibitor inhibitor inhibit