Potassium Channel Activator

A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.

Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K⁺ channel. Guanosine 5'-diphosphate is an iron mobilizer, which forms a complex with hepcidin to inhibit the hepcidin-ferroportin (FPN) interaction and modulates the IL-6/stat-3 pathway. Guanosine 5'-diphosphate ameliorates the Turpentine-induced anemia of inflammation (AI) in mice when combined with FeSO₄. Guanosine 5'-diphosphate can be used in the research of AI.

Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate 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-d₁₃ (GDP-d₁₃) dilithium is deuterium 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).

QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC₅₀ of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies.

Hydrochlorothiazid-¹³C,d₂ is the ¹³C- and deuterium labeled Hydrochlorothiazide. 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.

KCNQ1 activator-1 (compound 5) is a potent activator of KCNQ1 channel with an EC₅₀ of 1.69 μM. KCNQ1 activator-1 has the potential for the research of long QT syndrome (LQTS).

Paederosidic acid methyl ester is a ATP‐sensitive K⁺ channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K⁺ channel in the brain and spinal cord level.

3-Chlorodiphenylamine is a high affinity Ca²⁺ sensitizer of cardiac muscle. 3-Chlorodiphenylamine is based on diphenylamine and binds to the isolated N-domain of cardiac troponin C (cTnC) (K_d=6 µM). 3-Chlorodiphenylamine is an excellent starting scaffold for the development of more potent Ca²⁺-sensitizing compounds due to its small size, and can be used for systolic heart failure research.

Carabersat is a potent anticonvulsant agent.

Minocycline-d₆ sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.

Guanosine 5'-diphosphate (disodium salt) (Standard) is the analytical standard of Guanosine 5'-diphosphate (disodium salt). This product is intended for research and analytical applications. Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K+ channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI).

Uridine 5'-monophosphate-¹⁵N₂ (5'-​Uridylic acid-¹⁵N₂) is the ¹⁵N 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.

GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

Topiramate-13C6 (McN 4853-13C6) is the ¹³C labeled isotope of Topiramate (HY-B0122). 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.

Minocycline-d₇ is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.

11-Deoxyglycyrrhetinic acid sodium is a compound that exhibits anti-inflammatory activity. 11-Deoxyglycyrrhetinic acid sodium activates the Ca²⁺/voltage-gated K⁺ large conductance (BK) (cbv1 + β1) channels cloned from rat cerebral artery myocytes with the EC₅₀ of 53 μM.

Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium 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.

JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na⁺ channels and N-type Ca²⁺ channels, and is effective as a K⁺ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC₅₀=35 μM) and CA-I (18 μM).

NS-8, a pyrrole derivative, activates the Ca²⁺-sensitive k⁺-channel. NS-8 can suppress the micturition reflex by decreasing afferent pelvic nerve activity. NS-8 can be used in the research of urinary frequency and incontinence.