| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 3-cyano-4-(2-(1-methyl-1H-pyrazol-5-yl) phenoxy)-N-(thiazol-2-yl) benzenesulfonamide.
- CAS number: 1235397-05-3
- Molecular formula: C20H15N5O3S2.
- Purity: >98% (HPLC)
- Concentration: 10 nM - 1 µM.
- Form: Lyophilized powder.
- Solubility: 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. Repeat freeze-thawing may result in loss of activity.
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: NaV1.7 channels
- Source: Synthetic
- Activity: PF-04856264 is a blocker of NaV1.7 with an IC50 value of 28 nM for its inactivated state1.
Scientific background
Voltage-gated sodium (NaV) channels contribute to physiological and pathophysiological electrical signaling in nerve and muscle cells. The NaV1.7 is highly expressed on the exons somatic afferent neurons and is thought to play an important role in the signaling of inflammatory pain.PF-04856264, is a synthetic blocker of the human NaV1.7 channel. It has an effective concentration of 10 nM - 1 μM and an IC50 of 28 nM for NaV1.7 channel in its inactive state. NaV1.7 currents elicited by 20 ms depolarizing voltage steps from −120 mV are insensitive to inhibition by 1 µM PF-04856264, whereas the same concentration produced 91% ± 4% inhibition when a test pulse was preceded by an 8-s conditioning voltage step to inactivate approximately half of the channels. In contrast, NaV1.3 and NaV1.5 channels exhibit little or no sensitivity to inhibition by PF-04856264. Interestingly, different species orthologs exhibit different sensitivities to inhibition by PF. PF interacts with domain 4 voltage sensor M1,2,3 residues of the channel. When these extracellular residues are substituted with residues from the NaV1.3 channel the blocking effect of PF is abolished. Given the involvement of NaV in a variety of pathological conditions further research of subtype selective NaV channel inhibitors may prove useful for developing future therapeutic agents.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
