Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's plasma membrane. They are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials. Voltage-gated Na+ channels can exist in any of three distinct states: deactivated (closed), activated (open), or inactivated (closed). Ligand-gated sodium channels are activated by binding of a ligand instead of a change in membrane potential.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9540 |
Bliretrigine |
1233229-75-8 | Bliretrigine is a sodium channel blocker. Bliretrigine has the effect of relieving pain. |
H9478 |
Idrevloride |
1416973-63-1 | Idrevloride is a novel ,poent epithelial sodium channel (ENaC) inhibitor with IC50 values of 13.2 nM and 2.4 nM, resp. |
H9265 |
Nisoxetine hydrochloride |
57754-86-6 | Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM;Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels. |
H9264 |
PF-06305591 dihydrate |
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile. |
|
H9260 |
Lu AE98134 |
849000-18-6 | Lu AE98134 is a potent and selective positive modulator of NaV1.1 channels and also activates NaV1.6 channels;Lu AE98134 normalizes the altered firing properties of fast spiking interneurons (FSINs) in Dlx5/6+/- mice and can be used for the research of cognitive restoring in schizophrenia. |
H8996 |
TPC2-A1-P |
TPC2-A1-P is a powerful membrane-permeant Na+-selective two-pore channel 2 (TPC2) agonist. TPC2-A1-P activates a Na+ current and promotes endosome fusion with the plasma membrane. TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells. |
|
H8630 |
NS 383 |
309711-59-9 | NS383 inhibited H+‐activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC 50 values ranging from 0.61 to 2.2 μM; However, NS383 was completely inactive at homomeric ASIC2a. |
H8629 |
GX 201 |
1788071-27-1 | GX 201 is a potent and selective Nav1.7 blocker (IC50 = 3.2 nM). Exhibits 10x selectivity for Nav1.7 over Nav1.1, Nav1.2, and Nav1.6 channels; Displays prolonged residency time on the Nav1.7 channel. Chronic dosing increases compound potency ~10-fold and provides efficacy that persists after the compound has cleared from plasma. Suppresses neuropathic pain in a mouse diabetic neuropathy model. |
H8576 |
DS-1971a |
1450595-86-4 | DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects. |
H4825 |
XEN-907 |
912656-34-9 | A potent, selective NaV1.7 blocker with IC50 of 3 nM; shows no significant activity at 10 uM against a broad panel of 63 receptors and transporters; has no cytotoxic and favourable hepatocyte metabolic stability for both human and dog. |
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