Potassium Channel Activator

KCa1.1 channel activator-2 (compound 3F), a Quercetin hybrid derivative, is a selective vascular K_Ca1.1 channel stimulator. KCa1.1 channel activator-2 exhibits potent myorelaxant activity.

Minoxidil (U10858) hydrochloride is an ATP-sensitive potassium (K_ATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil hydrochloride is also a potent inhibitor of soybean lipoxygenaseare with an IC₅₀ of 20 μM.

Kv7 activator-2 (A14a) is a Kv7 potassium channel activator. Kv7 activator-2 can be used for the research of neurological disease, such as epilepsy.

Guanosine 5'-diphosphate-¹³C₁₀,¹⁵N₅ (GDP-¹³C₁₀,¹⁵N₅) dilithium is ¹³C and ¹⁵N-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K⁺ channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).

UR 8225 is an orally active ATP-sensitive K⁺ channel activator with vasodilator, smooth muscle relaxant, antihypertensive, and bronchodilator activities. UR 8225 induces membrane hyperpolarization by increasing outward K⁺ conductance and reduces Ca²⁺ influx through voltage-gated L-type Ca²⁺ channels. UR 8225 reduces total peripheral vascular resistance, shortens cardiac action potential duration, inhibits agonist-induced Ca²⁺ influx, and stimulates renin release. UR 8225 induces reflex tachycardia but lacks β-adrenergic receptor blocking activity. UR 8225 is widely applicable to research in fields related to hypertension, myocardial ischemia, ventricular fibrillation, and other conditions.

Unoprostone, a prostaglandin F2α analog, is a large conductance Ca²⁺-activated K⁺ (BK) channels and ClC-2 type chloride channels activator. Unoprostone reduces oxidative stress- and light-induced retinal cell death, and phagocytotic dysfunction. Unoprostone reduces intraocular pressure and can be used for the study of glaucoma, ocular hypertension and retinitis pigmentosa.

CAT335 is a TREK activator. CAT335 selectively and irreversibly activates TREK-1^CG∗. CAT335 can be used in the research of pain sensation, sleep, and intraocular pressure.

Hydrochlorothiazide-¹⁵N₂,¹³C,d₂ is ¹⁵N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.

PD-307243 is a hERG channel activator. PD-307243 can be used for research of arrhythmias.

Nigericin (sodium salt) (Standard) is the analytical standard of Nigericin (sodium salt). This product is intended for research and analytical applications. Nigericin sodium salt is an antibiotic derived from Streptomyces hygroscopicus that act as a K⁺/H⁺ ionophore, promoting K⁺/H⁺ exchange across mitochondrial membranes. Nigericin sodium salt is a NLRP3 activator. Nigericin sodium salt shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin sodium salt induces pyroptosis through caspase 1/GSDMD in TNBC.

Flupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride 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 hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

trans-AzoTAB is a photoresponsive potassium/sodium/calcium channel modulator and DNA-binding agent. trans-AzoTAB undergoes trans-cis isomerization driven by light, with variable polarity and DNA affinity. trans-AzoTAB also enhances voltage-gated potassium currents and inhibits sodium and calcium currents in cardiomyocytes, thereby reducing spontaneous electrical activity and excitation conduction velocity. In addition, trans-AzoTAB induces compaction and frozen conformation of λ-phage DNA, and non-sequence-dependently inhibits transcription and translation processes in the dark; its activity can be reversed and restored by visible light after activation with ultraviolet irradiation. trans-AzoTAB can serve as a probe for two-photon optical regulation of myocardial excitability, and is used to construct photoresponsive interfacial polymer structures.

Rosuvastatin lactone (Standard) is the analytical standard of Rosuvastatin lactone. This product is intended for research and analytical applications. Rosuvastatin lactone is a metabolite of Rosuvastatin (HY-17504A), a statin lipid-lowering agent and HMG-CoA inhibitor. Rosuvastatin lactone exhibits endothelium-independent and HMG-CoA reductase-independent vasorelaxant activity in rat aortic rings, and its vasorelaxant effect is jointly mediated by NO produced by inducible nitric oxide synthase (iNOS) located in vascular smooth muscle and activation of potassium channels. Rosuvastatin lactone itself has no lipid-lowering effect.

Flufenamic acid-d₄ is deuterium labeled Flufenamic acid. 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.

VU0405601 is a potent KV11.1 channel activator. VU0405601 protects cardiac tissue from dofetilide (HY-B0232)-induced ventricular tachycardia.

ZM226600 is an ATP-sensitive potassium channel opener (EC₅₀: 500 nM). ZM226600 inhibits bladder spontaneous activity.

KRN-2391 is a K_ATP channel opener with NO donor properties. KRN-2391 exerts dual inhibitory effects on overactive bladder (OAB) by activating KATP channels (causing cellular hyperpolarization and bladder smooth muscle relaxation) and releasing NO (enhancing relaxation via cGMP pathways). KRN-2391 is promising for research of OAB.

Kv7.2/Kv7.3 activator-4 (example 53) is a Kv7.2/Kv7.3 potassium channel activator that can be used in the research of epilepsy, neuropathic pain and other related diseases.

TMEM175 modulator 3 (Compound 14) is a TMEM175 modulator. TMEM175 modulator 3 can be used in research on neurodegenerative diseases.

Kv3 activator-1 is a Kv3 family voltage-gated potassium channel activator. Kv3 activator-1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and long-lasting, dose-related effects. Kv3 activator-1 can be used for the research of pain.