AZD3293 (Lanabecestat)

This product is for research use only, not for human use. We do not sell to patients.

AZD3293 (Lanabecestat)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$1350Check With Us
250mg$2380Check With Us
500mg$3570Check With Us

Cat #: V2701 CAS #: 1383982-64-6 Purity ≥ 98%

Description: Lanabecestat (formerly AZD-3293; LY-3314814; AZD3293; LY3314814) is a novel potent, orally bioactive, highly permeable, brain-penetreable inhibitor of beta-secretase 1 cleaving enzyme (BACE) with a Ki of 0.4 nM.

References: Eketjäll S, 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.

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Molecular Weight (MW)412.53
Molecular FormulaC26H28N4O
CAS No.1383982-64-6
Storage-20℃ for 3 years in powder formrr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 82 mg/mL (198.8 mM)rr
Water: <1 mg/mLrr
Ethanol: 82 mg/mL (198.8 mM)
Solubility In VivoLanabecestat; LY3314814; AZD3293; LY-3314814; AZD-3293; LY 3314814; AZD 3293
SynonymsNC(C(C)=N1)=NC21C3=C(C=CC(C4=CC(C#CC)=CN=C4)=C3)C[C@@]52CC[C@@H](OC)CC5
ProtocolIn VitroLanabecestat acts as a full inhibitor of BACE1 in vitro, with a competitive and reversible mechanism of action towards the hBACE1 active site. 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). The in vitro plasma protein binding of lanabecestat is determined by equilibrium dialysis using mouse, rat, guinea pig, dog, and human plasma. The compound is stable in the plasma of these species for at least the duration of the in vitro incubation period. The unbound fractions are 1.3% to 1.8% for mice, 4.2% to 5.9% for rats, 8.3% to 10.3% for guinea pigs, 9.4% to 10.3% for dogs, and 7.7% to 9.4% for human plasma. The mean blood:plasma ratio of 0.7 in human blood indicates no significant association with red blood cells. The free fraction in the brain tissue binding assay is 4.5%
In VivoIn 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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.4241 mL12.1203 mL24.2407 mL48.4813 mL
5mM0.4848 mL2.4241 mL4.8481 mL9.6963 mL
10mM0.2424 mL1.2120 mL2.4241 mL4.8481 mL
20mM0.1212 mL0.6060 mL1.2120 mL2.4241 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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:
  • (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.