Potassium Channel Activator

Siponimod (BAF-312) (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC₅₀ values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.

PD-118057 (Standard) is the analytical standard of PD-118057 (HY-108594). This product is intended for research and analytical applications. PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability.

SKA-31 (Standard) is the analytical standard of SKA-31. This product is intended for research and analytical applications. SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.

NS5806 (Standard) is the analytical standard of NS5806 (HY-108588). This product is intended for research and analytical applications. NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC₅₀ of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.

Flufenamic acid (Standard) is the analytical standard of Flufenamic acid. This product is intended for research and analytical applications. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca²⁺ channels, modulating non-selective cation channels (NSC), activating K⁺ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.

Cinnamyl Alcohol-d₅ is deuterated labeled Cinnamyl Alcohole (HY-Y0045). Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, exhibits anti-obesity, antioxidant and anti-inflammatory activities.

CLP257 (Standard) is the analytical standard of CLP257 (HY-110143). This product is intended for research and analytical applications. CLP257 is a selective K+-Cl cotransporter KCC2 activator with an EC₅₀ of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.

Dihydroisopimaric acid activates large conductance Ca²⁺ activated K⁺ (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.

Potassium ionophore III (BME-44) is a specific potassium ion carrier with high selectivity for sodium and ammonium ions and high lipophilicity.

Topiramate-¹³C (McN 4853-¹³C) is ¹³C labeled Topiramate. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

SG-209 is a Nicorandil (HY-B0341) derivative that produces relaxation through potassium channel activation, while this action contributes to the vasodilating action of Nicorandil (HY-B0341) at higher concentrations. SG-209 dilates tracheal smooth muscle and increases tracheal blood flow in anesthetized dogs.

ML213 (Standard) is the analytical standard of ML213 (HY-101843). This product is intended for research and analytical applications. ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC₅₀s of 230 and 510 nM, respectively.

KR-30450 (SKP 450) is a potent K⁺_ATP opener, and a potassium channel activator. KR-30450 exerts more potent cardioprotective effects than Lemakalim (HY-14255). KR-30450 significantly improves reperfusion cardiac function. KR-30450 significantly attenuates reperfusion contracture and lactate dehydrogenase release.

Levosimendan (Standard) is the analytical standard of Levosimendan. This product is intended for research and analytical applications. Levosimendan (Simsndan; OR-1259) is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.

NS3623 (Standard) is the analytical standard of NS3623 (HY-108586). This product is intended for research and analytical applications. NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.

ICA-069673 (Standard) is the analytical standard of ICA-069673 (HY-101396). This product is intended for research and analytical applications. ICA-069673 is a KCNQ2/Q3 potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC50s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guinea pig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells.

Topiramate-¹³C₆-1 (McN 4853-¹³C₆-1; RWJ 17021-¹³C₆-1) is ¹³C-labeled Topiramate (HY-B0122).

NS19504 (Standard) is the analytical standard of NS19504 (HY-110153). This product is intended for research and analytical applications. NS19504 is a Ca2+-activated K+ channel (BK channel, KCa1.1 channel) activator (EC₅₀=11.0 μM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.

Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

BL-1249 (Standard) is the analytical standard of BL-1249 (HY-108596). This product is intended for research and analytical applications. BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC₅₀ values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC₅₀ of 1.26 μM) than vascular tissue (EC₅₀ of 21.0 μM).