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

Lanabecestat  (Synonyms: AZD3293; LY3314814)

製品番号: HY-100740 純度: 99.87%
COA 取扱説明書 Technical Support

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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Lanabecestat

Lanabecestat 構造式

CAS 番号 : 1383982-64-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 在庫あり
Solution
10 mM * 1 mL in DMSO USD 275 在庫あり
Solid
2 mg $140 在庫あり
5 mg $250 在庫あり
10 mg $390 在庫あり
50 mg $1100 在庫あり
100 mg $1750 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 2 publication(s) in Google Scholar

Other Forms of Lanabecestat:

Lanabecestat 関連抗体

Top Publications Citing Use of Products

Beta-secretase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
BACE1 BACE2

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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[1].

IC50 & Target

BACE1

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.2 nM
Compound: 28
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
[PMID: 24704031]
体外実験

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.

Lanabecestat 関連抗体
体内実験

lanabecestat (5-25 mg/kg; p.o) displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ in mice, guinea pigs, and dogs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

412.53

分子式

C26H28N4O
CAS 番号
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 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

    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.
  • Protocol 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

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.87%

COA (250 KB) HNMR (282 KB) RP-HPLC (262 KB) LCMS (102 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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
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Lanabecestat Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

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

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