PF-04885614
Based on 1 Customer Validation
PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.00%
- No. CAS: 1480833-70-2
- Fòrmula: C13H14F3N3O
- Peso molecular:285.26
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuroprotective Compound Library
HY-L070
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Sodium Channel Blocker Library
HY-L118
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.053 μM
Compound: 13
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Inhibition of 50% inactivated recombinant human Nav1.8 expressed in HEK293 cells coexpressing Nav beta1 subunit at holding potential of -120 mV by manual patch electrophysiology method
Inhibition of 50% inactivated recombinant human Nav1.8 expressed in HEK293 cells coexpressing Nav beta1 subunit at holding potential of -120 mV by manual patch electrophysiology method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
1.8 μM
Compound: 13
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Inhibition of Cy3B-labeled ligand binding to recombinant human ERG expressed in HEK293 cells by fluorescence polarization method
Inhibition of Cy3B-labeled ligand binding to recombinant human ERG expressed in HEK293 cells by fluorescence polarization method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
11 μM
Compound: 13
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Inhibition of 50% inactivated recombinant human Nav1.1 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method
Inhibition of 50% inactivated recombinant human Nav1.1 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
16 μM
Compound: 13
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Inhibition of 50% inactivated recombinant human Nav1.2 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method
Inhibition of 50% inactivated recombinant human Nav1.2 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
2.6 μM
Compound: 13
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Inhibition of recombinant human ERG expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method
Inhibition of recombinant human ERG expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
27 μM
Compound: 13
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Inhibition of 50% inactivated recombinant human Nav1.5 expressed in HEK293 cells at holding potential of -150 mV by PatchXpress automated electrophysiology method
Inhibition of 50% inactivated recombinant human Nav1.5 expressed in HEK293 cells at holding potential of -150 mV by PatchXpress automated electrophysiology method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
4.2 μM
Compound: 13
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Inhibition of 50% inactivated recombinant human Nav1.6 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method
Inhibition of 50% inactivated recombinant human Nav1.6 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method
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10.1039/C6MD00281A |
| HEK293 | IC50 |
7 μM
Compound: 13
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Inhibition of 50% inactivated recombinant human Nav1.7 expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method
Inhibition of 50% inactivated recombinant human Nav1.7 expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method
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10.1039/C6MD00281A |
Chemical Information
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No. CAS 1480833-70-2
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Appearance Solid
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Peso molecular 285.26
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Fòrmula C13H14F3N3O
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Color Off-white to light yellow
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SMILES
NC(C)(C)C1=NC=C(C2=CC=C(OC(F)(F)F)C=C2)N1
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (876.39 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, 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.
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.
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 (7.29 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.29 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 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 (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.5056 mL | 17.5279 mL | 35.0557 mL | 87.6393 mL |
| 5 mM | 0.7011 mL | 3.5056 mL | 7.0111 mL | 17.5279 mL | |
| 10 mM | 0.3506 mL | 1.7528 mL | 3.5056 mL | 8.7639 mL | |
| 15 mM | 0.2337 mL | 1.1685 mL | 2.3370 mL | 5.8426 mL | |
| 20 mM | 0.1753 mL | 0.8764 mL | 1.7528 mL | 4.3820 mL | |
| 25 mM | 0.1402 mL | 0.7011 mL | 1.4022 mL | 3.5056 mL | |
| 30 mM | 0.1169 mL | 0.5843 mL | 1.1685 mL | 2.9213 mL | |
| 40 mM | 0.0876 mL | 0.4382 mL | 0.8764 mL | 2.1910 mL | |
| 50 mM | 0.0701 mL | 0.3506 mL | 0.7011 mL | 1.7528 mL | |
| 60 mM | 0.0584 mL | 0.2921 mL | 0.5843 mL | 1.4607 mL | |
| 80 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0955 mL | |
| 100 mM | 0.0351 mL | 0.1753 mL | 0.3506 mL | 0.8764 mL |
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