Potassium Channel Modulator

RA-2 is a negative-gating modulator of KCa2/3 channels with an IC₅₀ of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation.

Kv7.2/Kv7.3 modulator-3 (example 40 peak-1) is a selective K_v7.2/K_v7.3 modulator with an EC₅₀ of 0.099 μM.

AU-1421 is a potassium ion (K⁺) site-directed regulator that specifically acts on various cation transport ATPases. AU-1421 can distinguish between two different K⁺-sensitive phosphorylation intermediate (E2P) states: for non-K⁺ transport type ATPases (such as the sarcoplasmic reticulum Ca²⁺-ATPase), after binding to AU-1421, it mimics the agonistic effect of K⁺, significantly accelerating the hydrolysis (dephosphorylation) of E2P. For K⁺ transport type ATPases (such as the gastric mucosa H⁺/K⁺-ATPase and the renal Na⁺/K⁺-ATPase), after binding to AU-1421, it inhibits the hydrolysis of E2P, stabilizing the phosphorylated intermediate, thereby blocking the ion transport cycle. AU-1421 can be used to study the mechanism of the potassium ion pump.

Kv3 modulator 5 (Example 5) is a Kv3 channel modulator. Kv3 modulator 5 increases the Kv3.2 current. Kv3 modulator 5 can be used for research of hearing disorders.

Kv7.2 modulator 2 (compound 52) is a Kv7.2 channel modulator and can be used for study of epilepsy.

SDZ PCO 400 is a potassium channel modulator that relaxes airway smooth muscle and reverses airway obstruction caused by intravenous bronchospasmodics.

BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC₅₀ value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells.

MCC-134, a blocker of mitochondrial and opener of surface ATP-sensitive K+ (K_ATP) channels, abrogates cardioprotective effects of chronic hypoxia. MCC-134 is a vasorelaxing agent.

Kv7.2/Kv7.3 modulator-1 (compound 6a) is a Kv7.2/Kv7.3 modulator with the pEC₅₀ of 7.96 (KV7.2/3 channel opening activity). Kv7.2/Kv7.3 modulator-1 can be used for study of epilepsy, depression,brain injury and pain.

Kv7.2/Kv7.3 modulator-2 (compound 7d) is a Kv7.2/Kv7.3 modulator with the pEC₅₀ of 7.42 (KV7.2/3 channel opening activity). Kv7.2/Kv7.3 modulator-2 can be used for study of epilepsy, depression,brain injury and pain.

SK3 Channel-IN-1 (compound 7a) is a potent and specific SK3 channel modulator. SK3 Channel-IN-1 has efficient effect on breast cancer MDA-MB-435 cell migration while exhibiting low cytotoxicity in other cell lines. SK3 Channel-IN-1 can modulate ion channels’activity in cancer.

Tmem175 modulator 2 (example 180) is a TMEM175 modulator.Tmem175 modulator 2 can be used for the research of neurodegenerative disorders.

TMEM175 modulator 4 (Compound 3) is a TMEM175 modulator. TMEM175 modulator 4 modulates the activity of the lysosomal potassium channel TMEM175. TMEM175 modulator 4 can be used for research related to Parkinson's disease.

11-Deoxyprostaglandin F2α is an activator for TREK-2 channels with EC₅₀ of 0.294 μM. 11-Deoxyprostaglandin F2α inhibits the K2P channel TREK-1.

Kv7.2 modulator 1 (compound 10) is a Kv7.2 channel modulator and can be used for study of epilepsy.

AY 31906 is an orally active pyrimidine sulfonamide diuretic. AY 31906 exhibits potent diuretic and natriuretic activities in rats and dogs, along with relatively potassium-sparing properties. AY 31906 exhibits superior activity to Furosemide (HY-B0135). AY-31906 also has antihypertensive effects and can be used in the research of cardiovascular diseases.

HCN-IN-1 is a TLR4 inhibitor and HCN channel modulator with activity against HCN2 and HCN4.HCN-IN-1 inhibits TLR4-mediated alkaline phosphatase (SEAP) signal activity.HCN-IN-1 reduces HCN2 current across tested voltages, shifts voltage-dependent activation to more hyperpolarized potentials, slows activation kinetics, and does not affect deactivation process.HCN-IN-1 blocks HCN4 current.HCN-IN-1 exhibits analgesic, anti-inflammatory, and anti-anginal effects.HCN-IN-1 can be used for the research of inflammatory pain, neuropathic pain, heart failure, inflammation.

Maxi-K modulator 1 (Example 1) is a Maximum conductance calcium-activated potassium (Maxi-K) channel modulator. Maxi-K modulator 1 has a potent stimulating effect on Maxi-K channel activity. Maxi-K modulator 1 can be used for fragile X syndrome research.

Bepridil hydrochloride (Standard) (CERM 1978 (Standard);Org 5730 hydrochloride (Standard)) is the analytical standard of Bepridil hydrochloride (HY-103315). This product is intended for research and analytical applications. Bepridil hydrochloride is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

HARV-019 is a derivative of plant cannabinoids and belongs to sodium/potassium ion channel regulators or cannabinoid 1 receptor (b) regulators. HARV-019 can be used for the study of neurological diseases such as neuropathic pain and epilepsy.