channel block

N-type calcium channel blocker-1 is an orally active analgesic agent with a high affinity for functionally blocking N-type calcium channels.

M2 ion channel blocker ,Antiviral agent, is capable of inhibiting and blocking the activity of M2 ion channel.

NaV1.2/1.6 channel blocker-1 is a potent inhibitor of NaV1.2 and NaV1.6 channels, exhibiting inhibitory effects on rNaV1.6 and hNaV1.2. This compound can be utilized in the study of generalized epilepsy and movement disorders.

IEM 1754 2HBr (IEM 1754 dihydrobromide) is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

Norverapamil is a blocker of L-type calcium channel and an inhibitor of P-glycoprotein (P-gp) function .

Raxatrigine hydrochloride is a state-dependent sodium channel blocker and a Nav1.7 sodium channel inhibitor.

Lanicemine is a low-trapping NMDA channel blocker. It also has a binding (Ki: 0.56-2.1 μM).

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

Calcium channel-modulator-1, a calcium channel-modulator (IC50: 0.8 μM), specializes in blocking aortic constriction.

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

Paxilline is an indole alkaloid mycotoxin from *Penicillium paxilli*, acting as a potent BK channel inhibitor via an almost exclusively closed-channel block mechanism. Paxilline possesses significant anticonvulsant activity.

VU591 hydrochloride is a selective renal outer medullary potassium channel (Kir1.1, ROMK) antagonist (IC50:0.24 μM). Thought to block the intracellular pore of the Kir1.1 channel. Exhibits no effect on Kir7.1 at concentrations up to 10 μM; does not inhibi

MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n

Triamterene D5 is a deuterium-labeled Triamterene and can block epithelial Na+ channel (ENaC) in a voltage-dependent manner, used as a mild diuretic.

NeoSTX (Neosaxitoxin) is a specific sodium channel blocker that targets site 1. It works synergistically with local anesthetics to provide surgical anesthesia through peripheral nerve block or local infiltration and significantly prolongs postoperative analgesia duration.

Spadin Acetate is a natural peptide derived from a propeptide released in blood. Spadin Acetate is able to block the TREK-1 channel activity. Spadin Acetate binds specifically to TREK-1 with an affinity of 10 nM.

Detajmium is an anti-arrhythmia compound. It is an Na(+)-channel-blocking drug with an extremely long recovery from use-dependent sodium channel block.

NS-638 is a Ca2+-channel blocker. It can block K+-stimulated intracellular Ca2+-elevation (IC50: 3.4 μM).

Ropivacaine mesylate, a long-acting amide local anaesthetic, is used for spinal block and effectively mitigates neuropathic pain. It achieves analgesia by reversibly inhibiting sodium ion influx in nerve fibers, thus blocking impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes.

TRAM-34 (Triarylmethane-34) (Kd=20 nM), an effective and specific inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1), does not block cytochrome P450. The selective activity of TRAM-34(TRAM 34) is 200 to 1500-fold than other ion channels.

Relutrigine (PRAX-562) is an orally active, long-acting sodium current inhibitor that preferentially suppresses sustained INa induced by TX-II or SCN8A N1768D mutations (IC50=141/75 nM). It reduces neuronal intrinsic excitability and may be used for anticonvulsant therapy.

Glyburide-d11 is a deuterated form of Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor used in the study of diabetes and obesity. It inhibits P-glycoprotein and directly binds to block the SUR1 subunit of KATP, also inhibiting cystic fibrosis transmembrane conductance regulator (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing membrane ion permeability and can induce autophagy.

(-)-Epicatechin gallate (Standard) is a reference standard for research and analysis in studies involving (-)-Epicatechin gallate. (-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.