JNJ-61432059
Based on 1 publication(s) in Google Scholar
JNJ-61432059 is a blood-brain barrier-permeable, orally active TARP γ-8-associated AMPAR modulator with anticonvulsant activity. JNJ-61432059 negatively regulates GluA1 and positively modulates GluA2-containing AMPARs. JNJ-61432059 exerts potent protective effects in rodent epilepsy models. JNJ-61432059 is applicable for epilepsy-related research.
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- Pureza: 99.18%
- No. CAS: 2035814-50-5
- Fòrmula: C25H22FN5O2
- Peso molecular:443.47
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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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Publications Citing Use of MedChemExpress (MCE) JNJ-61432059
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Actividad biológica
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AMPA Receptor |
JNJ-61432059 (10 μM) potently inhibits glutamate-induced calcium flux in HEK-293 cells expressing GluA1o-γ-8 with a pIC50 of 9.7 ± 0.5, and shows no meaningful activity against HEK-293 cells expressing GluA1o-γ-2, with pIC50 < 5.0[1].
JNJ-61432059 (1-10 μM) has minimal cross-reactivity with a panel of 52 receptors, ion channels, and transporters at 1 μM, does not interact with hERG at 10 μM, and inhibits CYP 2C8 and CYP 2C9 with IC50 values of 3.0 μM and 1.9 μM, respectively[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.
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Animal Model:mice[1]
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Dosage:0.1, 1, 10, 100 mg/kg
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Administration:p.o., 5 days
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Result:Exerted anticonvulsant protection in the corneal kindling epilepsy model.
Chemical Information
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No. CAS 2035814-50-5
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Appearance Solid
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Peso molecular 443.47
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Fòrmula C25H22FN5O2
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Color White to off-white
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SMILES
OC1CCN(C2=NC=CC3=C(C4=CC=C(NC(C5)=O)C5=C4)C(C6=CC=C(F)C=C6)=NN32)CC1
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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 (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
2023 Mar 25;14(1):1659. PMID: 36966141
Solvente y solubilidad
DMSO : 50 mg/mL (112.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.08 mg/mL (4.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Savall BM, et al. Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators. ACS Med Chem Lett. 2018;10(3):267-272. Published 2018 Dec 26. [Content Brief]
[2]. Zhang D, et al. Modulatory mechanisms of TARP γ8-selective AMPA receptor therapeutics. Nat Commun. 2023;14(1):1659. Published 2023 Mar 25. [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 | 2.2549 mL | 11.2747 mL | 22.5494 mL | 56.3736 mL |
| 5 mM | 0.4510 mL | 2.2549 mL | 4.5099 mL | 11.2747 mL | |
| 10 mM | 0.2255 mL | 1.1275 mL | 2.2549 mL | 5.6374 mL | |
| 15 mM | 0.1503 mL | 0.7516 mL | 1.5033 mL | 3.7582 mL | |
| 20 mM | 0.1127 mL | 0.5637 mL | 1.1275 mL | 2.8187 mL | |
| 25 mM | 0.0902 mL | 0.4510 mL | 0.9020 mL | 2.2549 mL | |
| 30 mM | 0.0752 mL | 0.3758 mL | 0.7516 mL | 1.8791 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5637 mL | 1.4093 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4510 mL | 1.1275 mL | |
| 60 mM | 0.0376 mL | 0.1879 mL | 0.3758 mL | 0.9396 mL | |
| 80 mM | 0.0282 mL | 0.1409 mL | 0.2819 mL | 0.7047 mL | |
| 100 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5637 mL |
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