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Lanabecestat

Catalog No. TQ0238 CAS 1383982-64-6

Synonyms: LY3314814, AZD3293

Lanabecestat (AZD3293) is a highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor (Ki: 0.4 nM).

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Lanabecestat, CAS 1383982-64-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (242.41 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Susanna Eketjäll, et al. AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics. J Alzheimers Dis. 2016;50(4):1109-23.

Dose Conversion

You can also refer to dose conversion for different animals. More

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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The answer of 19.713 mg appears in the Mass box

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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

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.

Keywords

Lanabecestat 1383982-64-6 Neuroscience BACE LY3314814 AZD3293 Inhibitor inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.