2. Neuronal Signaling Cell Cycle/DNA Damage Autophagy
  3. Amyloid-β Dopamine Transporter CDK Autophagy
  4. TFEB activator 2

TFEB activator 2 is an orally active compound that can cross the blood-brain barrier. TFEB activator 2 can bind to the dopamine transporter (DAT). TFEB activator 2 promotes TFEB nuclear translocation and lysosome biogenesis by targeting the DAT-CDK9-TFEB pathway. TFEB activator 2 has neuroprotective activity and can be used in the research of Alzheimer's disease and other diseases.

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TFEB activator 2

TFEB activator 2 構造式

CAS 番号 : 3027414-04-3

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 330 在庫あり
Solution
10 mM * 1 mL in DMSO USD 330 在庫あり
Solid
5 mg $300 在庫あり
10 mg $480 在庫あり
25 mg $1000 在庫あり
50 mg $1600 在庫あり
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TFEB activator 2 関連抗体

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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製品説明

TFEB activator 2 is an orally active compound that can cross the blood-brain barrier. TFEB activator 2 can bind to the dopamine transporter (DAT). TFEB activator 2 promotes TFEB nuclear translocation and lysosome biogenesis by targeting the DAT-CDK9-TFEB pathway. TFEB activator 2 has neuroprotective activity and can be used in the research of Alzheimer's disease and other diseases[1].

体外実験

TFEB activator 2 (Compound 37) (10-30 μM; 3-6 h) promotes TFEB nuclear translocation in HeLa cells[1].
TFEB activator 2 (Compound 37) (10-30 μM; 6-24 h) promotes lysosome biogenesis and upregulates the expression of lysosomal and autophagic genes in HeLa cells[1].

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

TFEB activator 2 関連抗体

Real Time qPCR[1]

Cell Line: HeLa cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Increased the lysosomal genes of LAMP1, HEXA, CTSD and CTSF.
Increased the autophagic genes of LC3B, OPTN, p62, WIPI1 and ATG2A.
体内実験

TFEB activator 2 (Compound 37) (10 mg/kg; intraperitoneal injection; once every two days; 30 days) significantly reduces Aβ plaque burden in the hippocampus and cortex and improves learning and memory functions in APP/PS1 mice[1].

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

Animal Model: Five-month-old APP/PS1 mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; once every two days; 30 days
Result: Reduced Aβ plaque burden by 69.8% in the hippocampus and 29.5% in the cortex.
Decreased Aβ42 levels by 25.4% and 36.3% in the hippocampus and cortex, respectively.
Improved spatial learning and memory, as shown by reduced escape latency in the Morris Water Maze and increased platform crossings, and enhanced working memory in the Y maze.
Upregulated the expression of lysosomal and autophagic genes (e.g., LAMP1, CTSB) in the brain.
分子量

436.52

分子式

C26H29FN2O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC2=C(C=C1)NC=C2CCC3C4=C(CCN3CC5CCOCC5)C=C6OCOC6=C4
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 (229.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2908 mL 11.4542 mL 22.9085 mL
5 mM 0.4582 mL 2.2908 mL 4.5817 mL
10 mM 0.2291 mL 1.1454 mL 2.2908 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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Volume
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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

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体積 （開始）

V1

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濃度 （終了）

C2

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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: ≥ 5 mg/mL (11.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (11.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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mg/kg

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g

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(per animal)

μL

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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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+
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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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2908 mL 11.4542 mL 22.9085 mL 57.2711 mL
5 mM 0.4582 mL 2.2908 mL 4.5817 mL 11.4542 mL
10 mM 0.2291 mL 1.1454 mL 2.2908 mL 5.7271 mL
15 mM 0.1527 mL 0.7636 mL 1.5272 mL 3.8181 mL
20 mM 0.1145 mL 0.5727 mL 1.1454 mL 2.8636 mL
25 mM 0.0916 mL 0.4582 mL 0.9163 mL 2.2908 mL
30 mM 0.0764 mL 0.3818 mL 0.7636 mL 1.9090 mL
40 mM 0.0573 mL 0.2864 mL 0.5727 mL 1.4318 mL
50 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1454 mL
60 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9545 mL
80 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7159 mL
100 mM 0.0229 mL 0.1145 mL 0.2291 mL 0.5727 mL
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TFEB activator 2 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:

TFEB activator 23027414-04-3TFEB activator2TFEB activator-2Amyloid-βDopamine TransporterCDKAutophagyβ-amyloid peptideAβAbetaDATSLC6A3Cyclin dependent kinaseAlzheimer’s diseaselysosomeHela cellsSH-SY5Y cellAPP/PS1 miceInhibitorinhibitorinhibit

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製品番号:
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