PF-01247324
Based on 1 publication(s) in Google Scholar
PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
For research use only. We do not sell to patients.
- Purity: 99.77%
- CAS No.: 875051-72-2
- Formula: C13H10Cl3N3O
- Molecular Weight:330.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-01247324
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Biological Activity
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Nav1.8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.19 μM
Compound: 3
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Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology
Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology
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[PMID: 26101568] |
| HEK293 | IC50 |
12.8 μM
Compound: 3
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Inhibition of human Nav1.2 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.2 expressed in HEK293 cells by IonWorks Quattro selectivity assay
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[PMID: 26101568] |
| HEK293 | IC50 |
13 μM
Compound: 3
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Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay
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[PMID: 26101568] |
| HEK293 | IC50 |
19 μM
Compound: 3
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Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay
Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay
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[PMID: 26101568] |
| HEK293 | IC50 |
2.6 μM
Compound: 3
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Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
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[PMID: 26101568] |
| HEK293 | IC50 |
9 μM
Compound: 3
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Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay
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[PMID: 26101568] |
| SH-SY5Y | IC50 |
14 μM
Compound: 3
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Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
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[PMID: 26101568] |
| SH-SY5Y | IC50 |
14 μM
Compound: 3
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Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
|
[PMID: 26101568] |
| SH-SY5Y | IC50 |
14 μM
Compound: 3
|
Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
|
[PMID: 26101568] |
PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50=331 nM) and in recombinantly expressed h Nav1.8 channels (IC50=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC50=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50=10-18 μM). In vitro current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential[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.
Chemical Information
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CAS No. 875051-72-2
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Appearance Solid
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Molecular Weight 330.60
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Formula C13H10Cl3N3O
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Color Off-white to light yellow
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SMILES
O=C(C1=NC(N)=C(C2=CC(Cl)=CC(Cl)=C2Cl)C=C1)NC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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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Front Pharmacol
Mechanisms Underlying Gastrodin Alleviating Vincristine-Induced Peripheral Neuropathic Pain. [Abstract]2021 Dec 16:12:744663. PMID: 34975470
Solvent & Solubility
DMSO : ≥ 30 mg/mL (90.74 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: ≥ 2.5 mg/mL (7.56 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 (7.56 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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-
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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.
Protocol
Rats: For male Sprague Dawley rats (170-300 g), PF-01247324 is formulated as solutions of 0, 10, 30, 100 mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioural testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted[1].
Mice: PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of vehicle[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. [Content Brief]
[2]. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. [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 | 3.0248 mL | 15.1240 mL | 30.2480 mL | 75.6201 mL |
| 5 mM | 0.6050 mL | 3.0248 mL | 6.0496 mL | 15.1240 mL | |
| 10 mM | 0.3025 mL | 1.5124 mL | 3.0248 mL | 7.5620 mL | |
| 15 mM | 0.2017 mL | 1.0083 mL | 2.0165 mL | 5.0413 mL | |
| 20 mM | 0.1512 mL | 0.7562 mL | 1.5124 mL | 3.7810 mL | |
| 25 mM | 0.1210 mL | 0.6050 mL | 1.2099 mL | 3.0248 mL | |
| 30 mM | 0.1008 mL | 0.5041 mL | 1.0083 mL | 2.5207 mL | |
| 40 mM | 0.0756 mL | 0.3781 mL | 0.7562 mL | 1.8905 mL | |
| 50 mM | 0.0605 mL | 0.3025 mL | 0.6050 mL | 1.5124 mL | |
| 60 mM | 0.0504 mL | 0.2521 mL | 0.5041 mL | 1.2603 mL | |
| 80 mM | 0.0378 mL | 0.1891 mL | 0.3781 mL | 0.9453 mL |
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