49 products were found matching "K04841"!

Bupivacaine is a sodium channel blocker and local anesthetic. It inhibits sodium currents in rat dorsal horn neurons in a concentration-dependent manner and inhibits synaptic transmission in rat sympathetic ganglia, increasing the firing threshold when used at a concentration of 200 nM. Bupivacaine (10 µM) blocks...

Nav1.7 (Genbank # Q15858) is present at the endings of pain-sensing nerves, the nociceptors, close to region where the impulse is initiated. The Nav1.7 channel produces a rapidly activating and inactivating current which is sensitive to level of tetrodotoxin. Knockout mice that lack Nav1.7 in nociceptors showed...

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50s = 0.11-25 µM), L-type calcium, and KvLQT and hERG potassium channels (IC50s =...

Nav1.7 blocker 52 is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7, IC50 = 0.17 µM). It is selective for Nav1.7 over human-ether-a-go-go (hERG), also known as Kv11.1, Nav1.5, and Nav1.8 (IC50s = >10, 1.1, and 2.2 µM, respectively) but does inhibit Nav1.3 and Nav1.4 (IC50s = 0.3 and 0.4 µM, respectively)....

Carbamazepine is an inhibitor of sodium channels. It preferentially inhibits inactivated voltage-gated sodium channel Nav1.7 and Nav1.3 (IC50s = 406 and 900 µM, respectively) over resting (closed) Nav1.7 and Nav1.3 channels in whole-cell patch-clamp assays using HEK293 cells (IC50s = 1,584 and 2,464 µM,...

Protein function: Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical...

Anti-NAV1.7 Antibody was purified by Protein G chromatography. A BLAST analysis was used to suggest cross-reactivity with NAV1.7 from Human, Rat, and Mouse based on 100% homology with the immunizing sequence. No cross-reactivity against other Nav channels. Cross-reactivity with NAV1.7 from other sources has not been...

This gene encodes a voltage-gated sodium channel which plays a significant role in nociception signaling. Mutations in this gene have been associated with primary erythermalgia, channelopathy-associated insensitivity to pain, and paroxysmal extreme pain disorder. Protein function: Mediates the voltage-dependent...

Benzonatate is a reversible voltage-gated sodium channel blocker. It blocks Nav1.7 currents in a concentration- and voltage-dependent manner (IC50s = 5.9 and 1.4 µM at holding potentials of -100 and -70 mV, respectively) and inhibits action potential firing in catecholamine A differentiated (CAD) cells. Benzonatate...

This gene encodes a voltage-gated sodium channel which plays a significant role in nociception signaling. Mutations in this gene have been associated with primary erythermalgia, channelopathy-associated insensitivity to pain, and paroxysmal extreme pain disorder. Protein function: Mediates the voltage-dependent...

Tolperisone is a piperidine that acts as an inhibitor of voltage-gated sodium channels with an IC50 value of 198 µM, for inhibition of peak sodium currents evoked by step depolarizations in dorsal root ganglion (DRG) neurons, in vitro. Tolperisone acts as an antispastic agent that attenuates monosynaptic,...

Expectorant.