(E/Z)-J147
Based on 1 Customer Validation
(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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- Pureza: 99.54%
- No. CAS: 1146963-51-0
- Fòrmula: C18H17F3N2O2
- Peso molecular:350.34
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
MAO B; Dopamine transporter[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Cerebral cortex neuron | EC50 |
0.033 μM
Compound: J147
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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
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[PMID: 23582448] |
| Cortical neurone | EC50 |
25 nM
Compound: J147
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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
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[PMID: 32942072] |
| Hippocampal neurone | EC50 |
200 nM
Compound: J147
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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
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[PMID: 32942072] |
| HT-22 | EC50 |
0.02 μM
Compound: J147
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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
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[PMID: 23582448] |
(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.
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.
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Animal Model:24 male C57Bl/6 mice aged 24 months; using 8 month-old mice as controls[4]
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Dosage:200 ppm
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Administration:The diet was prepared by the addition of 200ppm; 6 months
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1146963-51-0
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Appearance Solid
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Peso molecular 350.34
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Fòrmula C18H17F3N2O2
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Color Off-white to pink
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SMILES
O=C(N(C1=CC=C(C)C=C1C)/N=C/C2=CC=CC(OC)=C2)C(F)(F)F
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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
Solvente y solubilidad
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.
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: ≥ 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.
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.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wang M, et al. The first synthesis of [11C]J147, a new potential PET agent for imaging of Alzheimer's disease. Bioorg Med Chem Lett. 2013 Jan 15;23(2):524-7. [Content Brief]
[2]. Prior M, et al. The neurotrophic compound J147 reverses cognitive impairment in aged Alzheimer's disease mice. Alzheimers Res Ther. 2013 May 14;5(3):25. [Content Brief]
[3]. Chen Q, et al. A novel neurotrophic drug for cognitive enhancement and Alzheimer's disease. PLoS One. 2011;6(12):e27865. [Content Brief]
[4]. Prior M, et al. Selecting for neurogenic potential as an alternative for Alzheimer's disease drug discovery. Alzheimers Dement. 2016 Jun;12(6):678-86. [Content Brief]
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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