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Sodium Channel

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Cat. No. Product Name Field of Application Chemical Structure
DC70685 PF-06526290 PF-06526290 is a potent, selective Nav1.3 inhibitor with IC50 of 5.1 uM, interact with the Domain 4 voltage sensor domain (D4 VSD and shows no activity for Nav1.7.
DC70706 PRAX-562 PRAX-562 (PRAX562) is a novel persistent sodium current (INa) inhibitor, inhibits hNaV1.6 persistent INa induced by ATX-II or SCN8A mutation N1768D with IC50 of 141 and 75 nM, respectively.PRAX-562 displays similar potency for inhibition of persistent INa expressed by other human NaV isoforms (hNaV1.1, hNaV1.2, hNaV1.5) as well as rat, dog, and mouse orthologs (rNaV1.2, dNaV1.2, mNaV1.6, rNaV1.6), with IC50 values ranging 109-180 nM.PRAX-562 exhibits tonic block with lower potency (IC50=8470 nM), demonstrating 60-fold preference for persistent INa, also exhibits preference for persistent INa over peak INa tonic block for hNaV1.1 (173-fold).PRAX-562 reduces intrinsic excitability of hippocampal CA1 pyramidal neurons without compromising action potential (AP) amplitude.PRAX-562 (3 mg/kg, po) produces dose-dependent protection (increase in latency) of mice against MES-induced tonic hindlimb seizures (EC50=90.1 ng/ml), with complete protection at 10 mg/kg.
DC70712 Psalmotoxin 1 Psalmotoxin 1 (PCTX1) is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker with IC50 of 0.9 nM.Psalmotoxin 1 displays no effect at ASIC1b, ASIC2a, ASIC3, heteromeric ASIC channels, ENaC and KV2.1/2.2/4.2/4.3 channels expressed in oocytes at 100 nM.Psalmotoxin 1 exhibits potent analgesic properties against thermal, mechanical, chemical, inflammatory and neuropathic pain in rodents.
DC70804 SSCI-1 SSCI-1 is a highly potent, selective NaV1.7 inhibitor with IC50 of 27 and 82 nM on human and rhesus Nav1.7 channels, respectively.SSCI-1 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 252 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-1 also exhibits high potency in manual patch clamp experiments (IC50=66/295 nM for huma/rhesus Nav1.7 channels).SSCI-1 does not affect myelinated nerve excitability as measured by TT, SSCI-1 inhibits odorant-induced olfaction in the olfactory bulb of rhesus monkeys, measured by fMRI.SSCI-1 inhibits withdrawal responses to noxious heat in rhesus monkeys.
DC70805 SSCI-2 Featured SSCI-2 is a highly potent, selective NaV1.7 inhibitor with IC50 of 9 and 17 nM on human and rhesus Nav1.7 channels, respectively.SSCI-2 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 183 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-2 also exhibits high potency in manual patch clamp experiments (IC50=24/62 nM for huma/rhesus Nav1.7 channels).SSCI-2 inhibits withdrawal responses to noxious heat in rhesus monkeys.
DC70647 Neurounina-1 Neurounina-1 is a small molecule Na+/Ca2+ exchanger (NCX) activator, stimulates NCX1 and NCX2 activities with EC50 of 1.1-2.7 nM, does not affect NCX3 activity.Neurounina-1 (10 nM) reduced cell death of primary cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation, also reduced γ-aminobutyric acid (GABA) release, enhanced GABA(A) currents, and inhibited both glutamate release and N-methyl-d-aspartate receptors in vitro.Neurounina-1 effectively protects against stroke damage in vivo.
DC70672 ORM-11372 Featured ORM‐11372 is a potent and highly selective NCX 1.1 inhibitor, inhibits human NCX 1.1 reverse and forward currents with IC50 of 5 and 6 nM respectively.ORM‐11372 weakly inhibits human cardiac sodium 1.5 (I Na) and hERG KV11.1 currents (I hERG) with IC50 of 23.2 and 10.0 uM.ORM‐11372 decreased both the outward and inward currents of hiPSC‐CMs with IC50 of 4.8 and 5.6 nM respectively, reduced the magnitude of outward I NCX (the reverse mode) in rat primary ventricular CMs with IC50 of 11.3 nM.ORM‐11372 concentration‐dependently inhibited the calcium efflux signa with an IC50 of 142 and 164 nM for experimental conditions increasing intracellular calcium and eliciting NCX forward mode activity, repectively.ORM‐11372 induced positive inotropic effects of 18 ± 6% and 35 ± 8% in anaesthetized rats with myocardial infarctions and in healthy rabbits respectively with no other haemodynamic effects.
DC70754 SAR296968 SAR296968 (SAR 296968) is a potent, selective Na+/Ca2+ exchanger (NCX) inhibitor, potently inhibits hNCX1/2/3 with IC50 of 74/23/129 nM, respectively.SAR296968 showed the same range of inhibitory potency on NCX1 orthologs from dog, guinea pig, pig, rabbit, and rat (IC50=20-200 nM).SAR296968 inhibited both the forward and reverse mode of the NCX current in a concentration-dependent manner with similarly high potency in voltage-clamp studies in guinea pig cardiomyocytes.SAR296968 displays little to no effect against 5-HT2B, benzodiazepine peripheral receptor, norepinephrine uptake, dopamine uptake, AR and PR.SAR296968 exhibited antiarrhythmic properties in animal models of arrhythmias related to early or late afterdepolarizations, significantly increased left ventricular contractility in anesthetized pigs.
DC70755 SAR340835 SAR340835 (SAR 340835, SAR296968 prodrug) is a potent, selective Na+/Ca2+ exchanger (NCX) inhibitor, a water-soluble prodrug of SAR296968.
DC71376 ABBV-318 Featured ABBV-318 is a potent Nav1.7/ Nav1.8 blocker, with IC50s of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. ABBV-318 can be used for the research of pain.
DC71377 Co 102862 Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na+ channel blocker. Co 102862 is also an orally active anticonvulsant.
DC72216 Pilsicainide Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent.
DC72364 4,9-Anhydrotetrodotoxin 4,9-Anhydrotetrodotoxin is a selective voltage-gated sodium channel (< a href=" " class="link-product" target="_blank">VGSC) inhibitor that blocks Nav1.1 and Nav1.6 in human brain and induces a hyperpolarizing shift in the voltage dependence of inactivated Nav1.6.
DC73678 Aneratrigine Aneratrigine is a sodium channel protein type 9 subunit alpha blocker.
DC73679 Benzocaine Benzocaine is a local anesthetic.
DC73680 BW-031 chloride BW-031 chloride is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.
DC73681 BW-031 iodide BW-031 iodide is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.
DC73682 DS43260857 DS43260857 is a potent, selective NaV1.7 inhibitor with IC50 of 15 nM (hNaV1.7), shows 440-fold and 930-fold selectivity over hNaV1.1 and hNaV1.5, respectively.
DC73683 LTGO-33 Featured LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.
DC73684 Tetrodotoxin Tetrodotoxin (TTx) is a potent, highly selective sodium channel blocker with IC50 of 33 nM for Nav1.6.
DC73685 UTX-143 UTX-143 is a potent, selective sodium-hydrogen exchange subtype 5 (NHE5) inhibitor with IC50 of 3.11 uM, 80-fold selective over NHE1.
DC73686 XPC-5462 XPC-5462 is a potent, selective dual inhibitor of NaV1.6 and NaV1.2 with IC50 of 10.9 nM and 10.3 nM, respectively.
DC73687 XPC-7224 XPC-7224 is a potent, selective NaV1.6 inhibitor with IC50 of 78 nM and 130 nM for human and mouse NaV1.6, respectively, interacts with the inactivated state of the channel.
DC74619 Ancistrotecine B Ancistrotecine B (Compound 2) is a Nav1.7 channel inhibitor (IC50: 0.73 μM). Ancistrotecine B relieves inflammatory pain in mice.
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