nav1.5

AZD 7009 is a novel antiarrhythmic compound that inhibits the sodium current of hNav1.5 in CHO K1 cells with an IC50 of 11 uM. AZD 7009 inhibited late sodium current in isolated rabbit atrial and ventricular myocytes, and prolonged E-4031-induced action potential duration, promoting early post-depolarization of Purkinye fibers (EADs).

Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

GNE-0439 is a novel Nav1.7-selective inhibitor (IC50: 0.34 uM) and inhibits Nav1.5 (IC50: 38.3 μM). GNE-0439 inhibits mutant N1742K channels (IC50: 0.37 uM) in membrane potential assays.

AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.

GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective positive modulator of Nav1.1 channels and also increases the activity of Nav1.2 and Nav1.5 channels while not affecting Nav1.4, Nav1.6, and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]

GDC-0310 is a selective acyl-sulfonamide inhibitor targeting the Na_v1.7 channel, with a potent inhibitory concentration (IC_50) of 0.6 nM against hNa_v1.7.

VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.

F 15845 is a blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. F15845 has been shown to selectively inhibit the persistent sodium current of Nav1.5[1] exerting cardioprotective effects following ischemia. In vitro testing showed minimal effects of F15845 on other important ion channels of the heart, including major Ca2+ and K+ channels.[1] This characteristic is thought to account for the limited effect of F15845 to change other heart parameters such as basal cardiac function, hemodynamic functions and ventricular fibrillation. F15845 was also shown to exert improved effects when the membrane potential was depolarized,[1] by acting on the extracellular side of the channel.

AA43279 is a novel selective Nav1.1 activator, increasing the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increasing the spontaneous inhibitory post-synaptic currents (sIPSCs) recorded from pyramidal neurons.

Flecainide acetate (R-818) is a class Ic antiarrhythmic agent used to prevent and treat tachyarrhythmias (abnormally fast heart rhythms).

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

Phrixotoxin 3 TFA is a potent inhibitor of voltage-gated sodium channels, with IC50 values of 0.6 nM for NaV1.2, 42 nM for NaV1.3, 72 nM for NaV1.4, 288 nM for NaV1.1, and 610 nM for NaV1.5. This compound modulates the activity of these channels similarly to traditional gating-modifier toxins, inducing a depolarizing shift in gating kinetics and obstructing the inward sodium current.

Phlo1b (μ-TrTx-Phlo1b), a 35-amino acid peptide toxin, selectively inhibits Nav1.7 channels with minimal inhibition of Nav1.2 and Nav1.5 [1].

Phlo1a (μ-TrTx-Phlo1a), a 35-amino acid peptide toxin, demonstrates a weak inhibitory effect on Nav1.2 and Nav1.5 channels [1]. Meanwhile, Phlo1b acts as a selective inhibitor of the Nav1.7 channel.

Ceratotoxin-1 (CcoTx1) is a peptide toxin that functions as an inhibitor of various voltage-gated sodium channel subtypes. It selectively inhibits Nav1.1 β1, Nav1.2 β1, Nav1.4 β1, and Nav1.5 β1 with IC50 values of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Additionally, Ceratotoxin-1 is known to inhibit Nav1.8 β1 [1].

Jingzhaotoxin XI (JZTX-XI) is a potent inhibitor of sodium conductance with an IC50 of 124 nM, and it significantly delays the rapid inactivation of Na_v1.5, with an EC50 of 1.18±0.2 μM, when expressed in Chinese hamster ovary (CHO-K1) cells [1].

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

Flecainide-d4 Acetate is a deuterated compound of Flecainide Acetate. Flecainide Acetate has a CAS number of 54143-56-5. Flecainide (acetate) is a class Ic antiarrhythmic agent used to prevent and treat tachyarrhythmias (abnormal fast rhythms of the heart).

Potent blocker of voltage-gated sodium channels (IC50 values are 0.6, 42, and 72 nM for NaV1.2, NaV1.3 and NaV1.5 respectively). Blocks inward sodium currents in a voltage-dependent manner.