1. Neuronal Signaling
  2. Beta-secretase
  3. Lanabecestat

Lanabecestat (Synonyms: AZD3293; LY3314814)

Cat. No.: HY-100740 Purity: 99.76%
Handling Instructions

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

For research use only. We do not sell to patients.

Lanabecestat Chemical Structure

Lanabecestat Chemical Structure

CAS No. : 1383982-64-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 227 In-stock
Estimated Time of Arrival: December 31
2 mg USD 140 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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

IC50 & Target

Ki: 0.4 nM (BACE1)[1]

In Vitro

Lanabecestat 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%[1].

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[1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (242.41 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4241 mL 12.1203 mL 24.2407 mL
5 mM 0.4848 mL 2.4241 mL 4.8481 mL
10 mM 0.2424 mL 1.2120 mL 2.4241 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female 7- to 14-week-old C57BL/6 mice (n=6 per treatment group and timepoint) receive 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

412.53

Formula

C₂₆H₂₈N₄O

CAS No.

1383982-64-6

SMILES

CC#CC1=CC(C2=CC([[email protected]@]34N=C(C)C(N)=N4)=C(C[[email protected]@]53CC[[email protected]@H](OC)CC5)C=C2)=CN=C1

Shipping

Room temperature in continental US; may vary elsewhere

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Lanabecestat
Cat. No.:
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Lanabecestat

Cat. No.: HY-100740