Potassium Channel Agonist

Atpenin A5 is a potent and highly specific complex II inhibitor (IC₅₀ ~10 nM), and is an effective mK_ATP channel agonist and cardioprotective agent.

2,2,2-Trichloroethanol, the active form of Chloral hydrate, is an agonist for the nonclassical K_2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

1-EBIO is an activator of Ca²⁺ sensitive K⁺ channels. 1-EBIO is used to study the role of K⁺ channels in diverse physiological functions.

Tetramisole hydrochloride is an orally active, selective inward rectifier potassium channel agonist with an EC₅₀ of approximately 30 μM for the Kir2.1 subunit. Tetramisole hydrochloride is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole hydrochloride promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole hydrochloride can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure.

ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC₅₀ of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects.

NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC₅₀s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

Naminidil is a cyanoguanidine K_ATP opener.

N-Arachidonoyl-L-serine (ARA-S) is an endocannabinoid. N-Arachidonoyl-L-serine induces phosphorylation of Akt and MAPK in endothelial cells. N-Arachidonoyl-L-serine also induces endothelium-dependent vasodilation in isolated rat mesenteric and abdominal aortas. N-Arachidonoyl-L-serine exhibits neuroprotective effects after traumatic brain injury by reducing apoptosis. N-Arachidonoyl-L-serine promotes the opening of KV7.1/KCNE1 channels in mammalian cells and shortens the action potential duration in cardiomyocytes. N-Arachidonoyl-L-serine may be used in research on cardiovascular and cerebrovascular diseases and neurological disorders.

Bimokalner (Bimokalnerum) is a voltage-gated potassium channel (Kv7.4) agonist.

TMEM175 agonist 2 is a TMEM175 agonist with an EC₅₀ of 0.0446 μM in human FLIPR assays and an EC₅₀ of 0.0453 μM in human TMEM175 EP assays. TMEM175 agonist 2 can be used in research related to Parkinson's disease, dementia with Lewy bodies, rapid eye movement sleep behavior disorder, amyotrophic lateral sclerosis, and lysosomal storage diseases.

2,2,2-Trichloroethanol (Standard) is the analytical standard of 2,2,2-Trichloroethanol. This product is intended for research and analytical applications. 2,2,2-Trichloroethanol, the active form of Chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

TMEM175 agonist 6 (Compound F-101) is a TMEM175 agonist. TMEM175 agonists can restore/enhance the function of lysosomes and reduce aSyn aggregation, thus being applicable for the research of diseases such as Parkinson's disease.

ZD-2767 is a selective ATP-sensitive potassium channel agonist. ZD-276 reduces cell membrane excitability and contractility by activating K_ATP channels in bladder smooth muscle. ZD-2767 is promising for research of overactive bladder.

A-278637 is a selective KATP channel opening agent with an EC₅₀ of 102 nM. A-278637 does not interact with other ion channels, including L-type calcium channels or other neurotransmitter receptor systems. A-278637 possesses a greater functional selectivity for urinary bladder versus vascular smooth muscle in vivo. A-278637 can be used for the study of overactive bladder.

Emakalim is an ATP-dependent potassium channel agonist. Emakalim can be used in the research of gliomas, triple-negative breast cancer, non-small cell lung cancer, and colorectal cancer.

TMEM175 agonist 1 is a TMEM175 agonist, with a human EC₅₀ of 0.378 μM in FLIPR assays and a human EC₅₀ of 0.886 μM in EP analyses. TMEM175 agonist 1 can be used in the research of Parkinson's disease, dementia with Lewy bodies, rapid eye movement sleep behavior disorder, amyotrophic lateral sclerosis, and lysosomal storage diseases.

KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of K_Ca2 channel. KCa2 channel modulator 1 potentiates human K_Ca2.3 channels with an EC₅₀ value of 0.19 μM and 0.99 μM on the rat K_Ca2.2 channel subtype.

TMEM175 agonist 7 is a TMEM175 agonist with an EC₅₀ of 543 nM. TMEM175 agonist 7 is applicable to the research of neurodegenerative diseases and lysosomal storage disorders.

SR 47063 is an ATP-sensitive potassium channel (K_ATP) agonist. SR 47063 selectively activates K_ATP channels in vascular smooth muscle cells (IC₅₀: 8.1 nM in human saphenous vein, 3.86 nM in rat aorta). SR 47063 promotes potassium efflux and cellular hyperpolarization to induce vasorelaxation. SR 4706 is promising for research of hypertension and related cardiovascular disorders.

TMEM175 agonist 5 (Compound 252) is a TMEM175 agonist with an EC₅₀ of 421 nM in FLIPR cell assays. TMEM175 agonist 5 can be used for the research of neurodegenerative diseases and lysosomal storage disorders.