Potassium Channel Activator

NS004 is a potassium (BK) channel activator that increases Iberiotoxin (HY-P0190) or Tetraethylammonium (HY-B1793)-sensitive whole-cell efflux currents. NS004 also significantly increased the activity of individual GH3 cell BK channels and rat brain BK channels reorganized into planar lipid bilayers, causing an increase in channel mean open time, a decrease in intermittent time, and an increase in channel voltage/calcium sensitivity.

GW542573X is a potent and selective Ca²⁺-activated K⁺ 2 (SK2) channels activator. GW542573X induces the Ca²⁺-response curve of hSK1 that left-shifted from an EC₅₀ (Ca²⁺) value of 410 nM to 240 nM.

BMS-191095 is a selective activator of mitochondrial ATP-sensitive potassium (mitoKATP) channels. BMS-191095 inhibits human platelet aggregation by opening mitochondrial K(ATP) channels.

Y-26763 is a K⁺ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K⁺ (K_ATP) channel activator.

VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC₅₀=165 nM) and GIRK1/4 (EC₅₀=720 nM) channels with improved brain penetration.

GoSlo-SR-5-69 is a potent activator of large conductance Ca²⁺-activated K⁺ (BK) channels, with an EC₅₀ of 251 nM.

IDOR-1104-0086 is an orally active K_v7 potassium channel opener with an EC₅₀ of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC₂₀ of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy.

Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K⁺ current, with ED₅₀ of 23 nM in the peptidergic caudodorsal neurons.

E0199 is a novel potent dual-target K_V7/Na_V modulator that activates the K_V7 channel (K_V7.2/7.3 (EC₅₀ = 12.78 nM), K_V7.2 (EC₅₀ = 0.50 μM), and K_V7.5 (EC₅₀ = 27.14 nM) channels) while simultaneously blocks the Na_V1.7 (IC₅₀ = 0.52 μM), Na_V1.8 (IC₅₀ = 0.24 μM), and Na_V1.9 (IC₅₀ = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research.

Topiramate (Standard) is the analytical standard of Topiramate. This product is intended for research and analytical applications. 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.

Guanosine 5'-diphosphate-¹⁵N₅ (GDP-¹⁵N₅) dilithium is 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).

Siponimod (BAF-312) hemifumarate 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 hemifumarate 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 hemifumarate can be used in research related to multiple sclerosis.

SKA-111 is a selective activator of potassium phannel K_Ca 3.1 , evokes K_Ca 3.1 membrane hyperpolarization in porcine endothelial cell. SKA-111 is capable of improving Bradykinin (HY-P0206)-induced coronary dilations in the isolated rat heart and can be used for cardiovascular disease research.

Flufenamic acid-¹³C₆ is the ¹³C₆ 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.

Guanosine 5'-diphosphate-¹³C₁₀ (GDP-¹³C₁₀) dilithium is ¹³C-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).

(±)-Naringenin (Standard) is the analytical standard of (±)-Naringenin. This product is intended for research and analytical applications. (±)-Naringenin is a naturally-occurring flavonoid. (±)-Naringenin displays vasorelaxant effect on endothelium-denuded vessels via the activation of BK_Ca channels in myocytes.

Saikogenin D is isolated from?Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca²⁺]i due to Ca²⁺ release from intracellular stores.

Uridine 5'-monophosphate-d₁₁ (5'- Uridylic acid-d₁₁) dilithium is deuterium labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.

AZSMO-23 is a potent hERG K⁺ channel activator. AZSMO-23 activats WT hERG pre-pulse and tail current with EC₅₀ values of 28.6, 11.2 µM, respectively. AZSMO-23 has the potential for the research of long QT syndrome.

CBIQ (4-Chlorobenzo[f]isoquinoline) is a benzoisoquinoline compound. CBIQ can activate the cystic fibrosis transmembrane conductance regulator (CFTR) Cl- ion channels and the intermediate-conductance calcium-sensitive K+ channel (KCNN4) with K_d values of 0.1 and 3.9 μM. CBIQ can be used for the research related to cystic fibrosis.