chemical

PF-04856264

P-265

P-265_10 mg

PF-04856264

Non Antibodies

S. Molecules

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

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

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.

Alomone Labs

NaV1.7 channels

PF-04856264 (#P-265) is a highly pure, synthetic, and biologically active compound.

A Specific Blocker of NaV1.7 Channel

437.5

Synthetic

C20H15N5O3S2.

10 nM - 1 µM.

PF-04856264 is a blocker of NaV1.7 with an IC50 value of 28 nM for its inactivated state1.

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.

50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Up to four weeks at 4°C or three months at -20°C.

1-2 Business Days

Israel/IL

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.

>98% (HPLC)

1235397-05-3

Lyophilized powder.

Contact Alomone Labs for technical support and product customization

41116134

Yes

3-cyano-4-(2-(1-methyl-1H-pyrazol-5-yl) phenoxy)-N-(thiazol-2-yl) benzenesulfonamide.