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

Lanabecestat  (Synonyms: AZD3293; LY3314814)

Cat. No.: HY-100740 Purity: 99.82%
COA Handling Instructions

Lanabecestat (AZD3293) est un inhibiteur puissant de la BACE1 pénétrant la barrière hémato-encéphalique avec un Ki de 0,4 nM.

Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease.

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
Solution
10 mM * 1 mL in DMSO USD 227 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 227 In-stock
Solid
2 mg USD 140 In-stock
5 mg USD 250 In-stock
10 mg USD 390 In-stock
50 mg USD 1100 In-stock
100 mg USD 1750 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lanabecestat:

Lanabecestat Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease[1].

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].

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

Lanabecestat Related Antibodies
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].

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

412.53

Appearance

Solid

Formula

C26H28N4O
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 5.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 6.

    Add each solvent one by one:  1% DMSO    99% saline

    Solubility: 0.5 mg/mL (1.21 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.82%

COA (251 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
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. 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
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Lanabecestat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

Keywords:

Lanabecestat1383982-64-6AZD3293 LY3314814AZD 3293AZD-3293LY3314814LY 3314814LY-3314814Beta-secretaseBACEβ-SecretaseInhibitorinhibitorinhibit

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