| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
NaV1.7 (voltage-gated sodium channel, SCN9A). PF-06456384 is a highly potent and selective inhibitor against voltage-gated sodium channel NaV1.7 with an IC50 of 0.01 nM for human NaV1.7. It shows IC50 values of <0.1 nM for mouse Nav1.7 and 75 nM for rat Nav1.7.
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| ln Vitro |
PF-06456384 is an extremely potent and selective Nav1.7 sodium channel blocker with an IC50 of 0.01 nM for hNaV1.7. It shows IC50 values of <0.1 nM for mNaV1.7 and 75 nM for rNaV1.7. Its high potency and selectivity for NaV1.7 make it a valuable tool for studying pain pathways.
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| ln Vivo |
PF-06456384 trihydrochloride has the potential for formalin pain model research. As a highly potent and selective NaV1.7 inhibitor, it can be used to study the role of NaV1.7 in pain sensation and to validate NaV1.7 as a therapeutic target for pain.
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| Enzyme Assay |
NaV1.7 channel inhibition assays are performed using automated patch-clamp electrophysiology in cells expressing human, mouse, or rat NaV1.7 channels. Voltage protocols are applied to activate sodium currents. PF-06456384 is applied at varying concentrations, and inhibition of sodium currents is measured. IC50 values are determined by non-linear regression analysis. Each concentration is tested in multiple cells. Selectivity is assessed against a panel of other ion channels and receptors.
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| Cell Assay |
Cellular NaV1.7 inhibition is evaluated in cell lines expressing NaV1.7 channels (e.g., HEK-293 cells). Cells are cultured in appropriate media and treated with PF-06456384 at various concentrations. Sodium currents are recorded using whole-cell patch-clamp electrophysiology. The compound's ability to inhibit sodium currents is assessed. Cell viability is assessed using MTT or LDH assays. Each experiment includes known NaV1.7 inhibitors as positive controls and vehicle controls.
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| Animal Protocol |
In vivo efficacy is evaluated in rodent models of pain, such as the formalin pain model. PF-06456384 is administered orally or intraperitoneally at doses determined by preclinical studies. Pain behaviors (licking, flinching) are assessed after formalin injection. The compound's ability to reduce pain behaviors is assessed. Pharmacokinetic parameters are assessed in parallel. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 829.18. Formula: C35H35Cl3F3N7O3S2. CAS No.: 1834610-75-1. Purity: 99.16%. Target: NaV1.7. For research use only.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available. As a NaV1.7 inhibitor, potential adverse effects may include altered pain perception and potential effects on other sodium channels at higher concentrations. Standard toxicity studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on the nervous system. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
PF-06456384 trihydrochloride is also known as PF-06456384. It is a highly potent and selective NaV1.7 inhibitor with an IC50 of 0.01 nM. It has potential for formalin pain model research. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C35H35CL3F3N7O3S2
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|---|---|
| Molecular Weight |
829.181712388992
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| Exact Mass |
719.195
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| CAS # |
1834610-75-1
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| Related CAS # |
PF-06456384;1834610-73-9
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| PubChem CID |
140810431
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
789.8±70.0 °C at 760 mmHg
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| Flash Point |
431.4±35.7 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.666
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| LogP |
6.95
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
53
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| Complexity |
1230
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CNCCC1CCNCC2=NC=CC(=C2)C3=C(C=CC(=C3)C4=CC(=CC=C4)C(F)(F)F)OC5=C(C=C(C=C5)S(=O)(=O)NC6=NC=NS6)C#N.Cl.Cl.Cl
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| InChi Key |
KUXFHGFSLKUFBC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H32F3N7O3S2.3ClH/c36-35(37,38)28-3-1-2-24(16-28)25-4-6-33(48-32-7-5-30(18-27(32)20-39)50(46,47)45-34-43-22-44-49-34)31(19-25)26-11-15-42-29(17-26)21-41-14-10-23-8-12-40-13-9-23;;;/h1-7,11,15-19,22-23,40-41H,8-10,12-14,21H2,(H,43,44,45);3*1H
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| Chemical Name |
3-cyano-4-[2-[2-[(2-piperidin-4-ylethylamino)methyl]pyridin-4-yl]-4-[3-(trifluoromethyl)phenyl]phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide;trihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~150.75 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2060 mL | 6.0301 mL | 12.0601 mL | |
| 5 mM | 0.2412 mL | 1.2060 mL | 2.4120 mL | |
| 10 mM | 0.1206 mL | 0.6030 mL | 1.2060 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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