Lanabecestat
Based on 2 publication(s) in Google Scholar
Lanabecestat (AZD3293; LY3314814) 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.
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- Pureza: 99.87%
- No. CAS: 1383982-64-6
- Fòrmula: C26H28N4O
- Peso molecular:412.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) Lanabecestat
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Actividad biológica
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BACE1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.2 nM
Compound: 28
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Inhibition of Fc domain of IgG1-fused human BACE (1 to 460) expressed in HEK293 cells preincubated for 10 mins followed by substrate addition measured after 15 mins by TR-FRET assay
Inhibition of Fc domain of IgG1-fused human BACE (1 to 460) expressed in HEK293 cells preincubated for 10 mins followed by substrate addition measured after 15 mins by TR-FRET assay
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[PMID: 24704031] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1383982-64-6
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Appearance Solid
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Peso molecular 412.53
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Fòrmula C26H28N4O
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Color White to off-white
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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
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Synonyms
AZD3293; LY3314814
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Neurogastroenterol Motil
Studying the Role of Myenteric Amyloidosis in Gastrointestinal Dysmotility and Enteric Neural Dysfunction Using APP/PS1 Mice-Is It an Adequate Animal Model?. [Abstract]2025 Sep;37(9):e70056. PMID: 40317839 -
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (242.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.21 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4241 mL | 12.1203 mL | 24.2407 mL | 60.6017 mL |
| 5 mM | 0.4848 mL | 2.4241 mL | 4.8481 mL | 12.1203 mL | |
| 10 mM | 0.2424 mL | 1.2120 mL | 2.4241 mL | 6.0602 mL | |
| 15 mM | 0.1616 mL | 0.8080 mL | 1.6160 mL | 4.0401 mL | |
| 20 mM | 0.1212 mL | 0.6060 mL | 1.2120 mL | 3.0301 mL | |
| 25 mM | 0.0970 mL | 0.4848 mL | 0.9696 mL | 2.4241 mL | |
| 30 mM | 0.0808 mL | 0.4040 mL | 0.8080 mL | 2.0201 mL | |
| 40 mM | 0.0606 mL | 0.3030 mL | 0.6060 mL | 1.5150 mL | |
| 50 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2120 mL | |
| 60 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0100 mL | |
| 80 mM | 0.0303 mL | 0.1515 mL | 0.3030 mL | 0.7575 mL | |
| 100 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6060 mL |
Lanabecestat Related Classifications
HY-100740 Related Classifications
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