2. Neuronal Signaling
  3. Monoamine Oxidase Dopamine Transporter
  4. (E/Z)-J147

(E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the study of Alzheimer’s disease (AD).

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(E/Z)-J147

(E/Z)-J147 構造式

CAS 番号 : 1146963-51-0

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $70 在庫あり
25 mg $110 在庫あり
50 mg $160 在庫あり
100 mg $240 在庫あり
500 mg $597 在庫あり
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Based on 0 publication(s) in Google Scholar

Other Forms of (E/Z)-J147:

(E/Z)-J147 関連抗体

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Monoamine Oxidase 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
MAO-A MAO-B

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  • 純度とドキュメンテーション

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製品説明

(E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the study of Alzheimer’s disease (AD)[1][2][3].

IC50 & Target

MAO B; Dopamine transporter[2]
Cellular Effect
Cell Line Type Value Description References
Cerebral cortex neuron EC50
0.033 3
Compound: J147
Neuroprotective activity in rat primary cortical neurons assessed as reduction in trophic factor withdrawal after 2 days by fluorescent live-dead assay
Neuroprotective activity in rat primary cortical neurons assessed as reduction in trophic factor withdrawal after 2 days by fluorescent live-dead assay
[PMID: 23582448]
Cerebral cortex neuron EC50
0.033 3
Compound: J147
Neuroprotective activity in rat primary cortical neurons assessed as reduction in trophic factor withdrawal after 2 days by fluorescent live-dead assay
Neuroprotective activity in rat primary cortical neurons assessed as reduction in trophic factor withdrawal after 2 days by fluorescent live-dead assay
[PMID: 23582448]
HT-22 EC50
0.02 3
Compound: J147
Neuroprotective activity in mouse HT22 cells assessed as reduction in glutamate-induced oxidative stress incubated for 30 mins prior to glutamate-challenge measured after 24 hrs by MTT assay
Neuroprotective activity in mouse HT22 cells assessed as reduction in glutamate-induced oxidative stress incubated for 30 mins prior to glutamate-challenge measured after 24 hrs by MTT assay
[PMID: 23582448]
Cortical neurone EC50
25 1
Compound: J147
Neuroprotective activity against rat Primary cortical neuron cells assessed as rescue of cell death incubated for 2 days by fluorescent live-dead assay
Neuroprotective activity against rat Primary cortical neuron cells assessed as rescue of cell death incubated for 2 days by fluorescent live-dead assay
[PMID: 32942072]
Hippocampal neurone EC50
200 1
Compound: J147
Neuroprotective activity against amyloid beta induced cell death in rat Primary hippocampal neuron cells assessed as increase in cell viability incubated for 2 days by lactate dehydrogenase release assay
Neuroprotective activity against amyloid beta induced cell death in rat Primary hippocampal neuron cells assessed as increase in cell viability incubated for 2 days by lactate dehydrogenase release assay
[PMID: 32942072]
Cortical neurone EC50
25 1
Compound: J147
Neuroprotective activity against rat Primary cortical neuron cells assessed as rescue of cell death incubated for 2 days by fluorescent live-dead assay
Neuroprotective activity against rat Primary cortical neuron cells assessed as rescue of cell death incubated for 2 days by fluorescent live-dead assay
[PMID: 32942072]
HT-22 EC50
0.02 3
Compound: J147
Neuroprotective activity in mouse HT22 cells assessed as reduction in glutamate-induced oxidative stress incubated for 30 mins prior to glutamate-challenge measured after 24 hrs by MTT assay
Neuroprotective activity in mouse HT22 cells assessed as reduction in glutamate-induced oxidative stress incubated for 30 mins prior to glutamate-challenge measured after 24 hrs by MTT assay
[PMID: 23582448]
Hippocampal neurone EC50
200 1
Compound: J147
Neuroprotective activity against amyloid beta induced cell death in rat Primary hippocampal neuron cells assessed as increase in cell viability incubated for 2 days by lactate dehydrogenase release assay
Neuroprotective activity against amyloid beta induced cell death in rat Primary hippocampal neuron cells assessed as increase in cell viability incubated for 2 days by lactate dehydrogenase release assay
[PMID: 32942072]
体外実験

(E/Z)-J147 promotes HT22 and primary cell survival in a dose-dependent manner (EC50 value range of 0.06-0.115 μM) [2].

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

(E/Z)-J147 関連抗体
体内実験

(E/Z)-J147 (diet is prepared by the addition of (E/Z)-J147 at 200ppm; 6 months) enhances memory and dendritic spine number in old mice[4].
The half life (t1/2) of (E/Z)-J147 is calculated at 1.5 hrs in plasma and 2.5 hrs in brain ( per oral (PO) administration at a single dose of 20 mg/kg)[2].

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

Animal Model: 24 male C57Bl/6 mice aged 24 months; using 8 month-old mice as controls[4]
Dosage: 200 ppm
Administration: The diet was prepared by the addition of 200ppm; 6 months
Result: While both young and old animals recognized when an object was moved a large distance (135 degrees), a reduction in the recognition index (RI) in aged mice was observed when the object was moved a smaller distance of 45 degrees. The reduction in the RI was reversed upon treatment with (E/Z)-J147.
臨床実験
分子量

350.34

分子式

C18H17F3N2O2
CAS 番号
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(N(C1=CC=C(C)C=C1C)/N=C/C2=CC=CC(OC)=C2)C(F)(F)F
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 (285.44 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 2.8544 mL 14.2718 mL 28.5437 mL
5 mM 0.5709 mL 2.8544 mL 5.7087 mL
10 mM 0.2854 mL 1.4272 mL 2.8544 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)

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

一般には略語で表示されます：C1V1 = C2V2

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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: ≥ 1.88 mg/mL (5.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.88 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.8 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: 1.88 mg/mL (5.37 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.88 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.8 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:

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mg/kg

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g

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(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: 99.54%

COA (248 KB) LCMS (114 KB)

取扱説明書 (2659 KB)
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 2.8544 mL 14.2719 mL 28.5437 mL 71.3593 mL
5 mM 0.5709 mL 2.8544 mL 5.7087 mL 14.2719 mL
10 mM 0.2854 mL 1.4272 mL 2.8544 mL 7.1359 mL
15 mM 0.1903 mL 0.9515 mL 1.9029 mL 4.7573 mL
20 mM 0.1427 mL 0.7136 mL 1.4272 mL 3.5680 mL
25 mM 0.1142 mL 0.5709 mL 1.1417 mL 2.8544 mL
30 mM 0.0951 mL 0.4757 mL 0.9515 mL 2.3786 mL
40 mM 0.0714 mL 0.3568 mL 0.7136 mL 1.7840 mL
50 mM 0.0571 mL 0.2854 mL 0.5709 mL 1.4272 mL
60 mM 0.0476 mL 0.2379 mL 0.4757 mL 1.1893 mL
80 mM 0.0357 mL 0.1784 mL 0.3568 mL 0.8920 mL
100 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7136 mL
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(E/Z)-J147 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 *
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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:

(E/Z)-J1471146963-51-0Monoamine OxidaseDopamine TransporterMAODATSLC6A3BBBmonoamineoxidaseMAO BdopamineAlzheimer diseaseneuroprotectiveInhibitorinhibitorinhibit

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製品名:
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製品番号:
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