channel

Tetracaine hydrochloride (Amethocalne HCl) (Pontocaine), a potent local anaesthetic, is a channel function allosteric inhibitor. It is primarily used as an antipruritic and topically in ophthalmology, and it has been used for surface and spinal anesthesia.

2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4). It activates a nonclassical potassium channel in cerebrovascular smooth muscle and dilates the middle cerebral artery [1]. [1]. Nikhil K Parelkar, et al. 2,2,2-trichloroethanol Activates a Nonclassical Potassium Channel in Cerebrovascular Smooth Muscle and Dilates the Middle Cerebral Artery. J Pharmacol Exp Ther. 2010 Mar;332(3):803-10.

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.

Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM), as well as an effective mKATP channel agonist and cardioprotective agent [1].

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

Calcium Channel antagonist 4 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Calcium Channel antagonist 3 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 (EC50s: 14.23 μM and 3.34 μM) and is used as a potential treatment for motor nerve terminal dysfunction.

Potassium Channel Activator 1 can be used in studies about the treatment of disorders or conditions wherein the dopaminergic system is disrupted such as mood disorders ADHD, schizophrenia, and other psychotic states.

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

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

Sodium Channel inhibitor1 is a novel and selective voltage-gated sodium channel for pain treatment. (IC50 Value of 0.16 uM and 0.41 uM for Na v1.7, V hold-90mV and Na v1.7, V hold-90mV)

Sodium Channel Inhibitor 2 [Sodium Channel inhibitor 2] is a blocker of sodium channels.

Calcium Channel antagonist5 (compound 32) is a calcium channel antagonist with a pIC50 of 5.50.

Sodium Channel inhibitor6 (compound I) is a sodium channel inhibitor utilized in the study of neuropathic pain.

KCa2 channel modulator 1 (compound 2o) is an effective, subtype-selective K Ca2 channel positive modulator that potentiates rat KCa2.2 channels with an EC50 value of 0.99 μM and human KCa2.3 channels with an EC50 value of 0.19 μM [1].

KCa2 channel modulator 2 (compound 2q) is an effective, subtype-selective K Ca 2 channel positive modulator with similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, exhibiting EC50 values of 0.60 μM and 0.64 μM, respectively [1].

SK3 Channel-IN-1 (compound 7a) is a potent and selective SK3 channel modulator that effectively inhibits breast cancer MDA-MB-435 cell migration with low cytotoxicity in other cell lines, and it modulates ion channel activity in cancer cells [1].

T-Type calcium channel inhibitor 2 (compound 6g) is a potent inhibitor of the T-type calcium channel, specifically acting on Cav3.1 (α1G) with an IC50 of 31.0 μM, Cav3.2 (α1H) with an IC50 of 83.1 μM, and Cav3.3 (α1I) (α1H). T-Type calcium channel inhibitor 2 exhibited cytotoxicity against A549 and HCT-116 cells with IC50s of 5.0 μM and 6.4 μM, respectively.

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.

KCa1.1 Channel Activator-1, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels while also blocking CaV1.2 channels. Additionally, it demonstrates weak myorelaxant activity.

KCa1.1 channel activator-2, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels. This compound demonstrates significant myorelaxant activity.

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

Nav1.3 Channel Inhibitor 1 (Compound 15b) is a state-dependent inhibitor of the voltage-gated sodium channel Na v 1.3, with an IC50 value of 20 nM. It has the ability to cross the blood-brain barrier, making it applicable for research into nervous system disorders [1].