PF-04856264
Based on 1 publication(s) in Google Scholar
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.
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- Pureza: 99.29%
- No. CAS: 1235397-05-3
- Fòrmula: C20H15N5O3S2
- Peso molecular:437.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Publications Citing Use of MedChemExpress (MCE) PF-04856264
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Actividad biológica
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Nav1.7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 1a; PF-04856264
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Inhibition of human Nav1.5 expressed in HEK293 cells at -140 mV holding potential measured for 8 secs by patch-clamp method
Inhibition of human Nav1.5 expressed in HEK293 cells at -140 mV holding potential measured for 8 secs by patch-clamp method
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[PMID: 28389149] |
| HEK293 | IC50 |
0.2 μM
Compound: 18; PF-04856264
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Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp method
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp method
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[PMID: 28629594] |
| HEK293 | IC50 |
28 nM
Compound: 17, PF-04856264
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Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay
Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay
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[PMID: 25927480] |
| HEK293 | IC50 |
28 nM
Compound: 1a; PF-04856264
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Inhibition of human Nav1.7 expressed in HEK293 cells at -120 mV holding potential measured for 8 sec by patch-clamp method
Inhibition of human Nav1.7 expressed in HEK293 cells at -120 mV holding potential measured for 8 sec by patch-clamp method
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[PMID: 28389149] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks adult male C57BL/6J mice (OD1-induced spontaneous pain model)[2]
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Dosage:3, 30 mg/kg
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Administration:I.p.
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Result:Significantly reduced spontaneous pain behaviors in mice.
Chemical Information
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No. CAS 1235397-05-3
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Appearance Solid
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Peso molecular 437.49
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Fòrmula C20H15N5O3S2
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Color Off-white to light yellow
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SMILES
O=S(C1=CC=C(OC2=CC=CC=C2C3=CC=NN3C)C(C#N)=C1)(NC4=NC=CS4)=O
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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
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 250 mg/mL (571.44 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 2.5 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (277 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc Natl Acad Sci U S A. 2013;110(29):E2724-E2732. [Content Brief]
[2]. Deuis JR, et al. Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain. Toxins (Basel). 2016;8(3):78. Published 2016 Mar 17. [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, 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 | 2.2858 mL | 11.4288 mL | 22.8577 mL | 57.1442 mL |
| 5 mM | 0.4572 mL | 2.2858 mL | 4.5715 mL | 11.4288 mL | |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2858 mL | 5.7144 mL | |
| 15 mM | 0.1524 mL | 0.7619 mL | 1.5238 mL | 3.8096 mL | |
| 20 mM | 0.1143 mL | 0.5714 mL | 1.1429 mL | 2.8572 mL | |
| 25 mM | 0.0914 mL | 0.4572 mL | 0.9143 mL | 2.2858 mL | |
| 30 mM | 0.0762 mL | 0.3810 mL | 0.7619 mL | 1.9048 mL | |
| 40 mM | 0.0571 mL | 0.2857 mL | 0.5714 mL | 1.4286 mL | |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4572 mL | 1.1429 mL | |
| 60 mM | 0.0381 mL | 0.1905 mL | 0.3810 mL | 0.9524 mL | |
| 80 mM | 0.0286 mL | 0.1429 mL | 0.2857 mL | 0.7143 mL | |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5714 mL |
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