Potassium Channel Activator

Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K+ (KATP) channels in guinea pig ventricular myocytes. Using patch-clamp techniques, it was found that aprikalim enhances KATP channel activity more effectively in Mg-NDP solution compared to standard solutions. In Mg-NDP solution, aprikalim reduced the sensitivity of KATP channels to ATP, increasing the concentration of ATP required to inhibit channel activity by half (K1) from 56 μM to 180 μM. However, this effect diminished over time. Aprikalim's ability to activate KATP channels in Mg-NDP solution suggests potential therapeutic implications in modulating cardiac excitability and may relate to changes in channel protein enzymatic activity under experimental conditions.

4-Octyl itaconate-Bn-S-NH2 (Compound 8b) is a vasodilator. 4-Octyl itaconate-Bn-S-NH2 can slowly and stably release H₂S, and it alleviates oxidative stress through an antioxidant reaction that depends on the activation of Nrf2. 4-Octyl itaconate-Bn-S-NH2 inhibits the production of intracellular ROS caused by H₂O₂ damage and the cytotoxicity of cells, and activates potassium channel. 4-Octyl itaconate-Bn-S-NH2 can be used for research on hypertension.

Ebio2 is a potent KCNQ2 activator.

Procainamide (Standard) is the analytical standard of Procainamide. This product is intended for research and analytical applications. Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research.

VU0494372 is an activator of potassium ion channel KCNQ1. VU0494372 can significantly enhance the cell surface expression and transport efficiency of KCNQ1. VU0494372 does not alter KCNQ1 mRNA levels and protein degradation rate, and has no significant cytotoxicity. VU0494372 can be used for research on cardiovascular conditions.

Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC₅₀: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models.

KMUP-4, as a xanthine derivative with cGMP-enhancing activity, induces aortic relaxation through endothelium-dependent and independent mechanisms. KMUP-4 increases cytoplasmic cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterases (PDEs) and activating K⁺ channels. KMUP-4 can be used in the study of cardiovascular diseases.

Uridine 5'-monophosphate (disodium salt) (Standard) is the analytical standard of Uridine 5'-monophosphate (disodium salt). This product is intended for research and analytical applications. Uridine 5'-monophosphate (5'-Uridylic acid) disodium salt is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate disodium salt can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.

Kv3.1 activator-1 is a Kv3.1 voltage-gated potassium channel activator. Kv3.1 activator-1 exhibits distinct activating efficacy in both thallium flux assays and automated patch-clamp electrophysiological assays .

Kv3.1 activator-2 is a Kv3.1 voltage-gated potassium channel (potassium channel) activator with concentration-dependent activity. Kv3.1 activator-2 opens Kv3.1 potassium channels, increases channel current amplitude, and exerts a positive channel activation effect. Kv3.1 activator-2 can be used in the research of neurological diseases.

P-1060 is a potassium channel opener. P-1060 can be used for the research of cardiovascular disease.

KMUP-1 is a xanthine derivative with vasodilator activity. KMUP-1 is a inhibitor of phosphodiesterase (PDE) and activator of soluble guanylyl cyclase (sGC). KMUP-1 stimulates NO/sGC/cyclic GMP pathway. KMUP-1 has K⁺ channels opening activity. KMUP-1 ameliorates ischemia-induced cardiomyocyte apoptosis. KMUP-1 can be used for cardiovascular and anti-inflammatory study.

Cetiedil citrate is a vasodilator and antihemolytic agent. Cetiedil citrate exerts anti-sickle cell anemia effects by blocking Ca²⁺-activated K⁺ channels (Gardos/KCa3.1). Cetiedil citrate is a muscarinic receptor antagonist that inhibits calcium-dependent release of acetylcholine (ACh) from mediated reconstituted proteoliposomes, with a K_i value of 5 μM. Cetiedil citrate possesses analgesic, spasmolytic and local anesthetic activities. Cetiedil citrate can be used in research related to ischemic leg pain caused by vascular diseases and sickle cell disease.

KR-31378 is a neuroprotectant with dose-dependent pharmacokinetic properties and relevant activity in rats. After intravenous and oral administration of KR-31378 in rats, its pharmacokinetic parameters showed dose-dependent changes, such as decreased clearance with increasing doses, good oral absorption, and comparable AUCs for intravenous and oral administration at different doses.

Fluoxakalner is a selective Kv7.2/7.3 channel opener with an EC₅₀ of 0.36 μM. Fluoxakalner accelerates the activation kinetics of Kv7.2/7.3 channels and produces anti-nociceptive effects. Fluoxakalner is applicable for pain research.

KCa1.1 channel activator-1 (compound 1E), a Quercetin hybrid derivative, is a selective vascular K_Ca1.1 channel channel stimulator. KCa1.1 channel activator-1 also displays Ca_V1.2 channel blocking activity. KCa1.1 channel activator-1 exhibits weak myorelaxant activity.

E0714 is a blood-brain barrier-permeable, selective Kv7.2 potassium channel activator, with EC₅₀ values of 1.90 μM and 0.021 μM for homotetrameric Kv7.2 channels and heterotetrameric Kv7.2/7.3 channels, respectively. E0714 exhibits anticonvulsant activity. E0714 can be used in research related to epilepsy.

7-epi-Taxol (Standard) is the analytical standard of 7-epi-Taxol. This product is intended for research and analytical applications. 7-epi-Taxol is an active metabolite of taxol, with activity comparable to that of taxol against cell replication, promoting microtubule bundle formation and against microtubule depolymerization.

Kv7.2/Kv7.3 activator-1 (compound 517) is a potent Kv7.2/Kv7.3 channel activator with an EC₅₀ value of ＜1 µM. Kv7.2/Kv7.3 activator-1 has the potential for the research of neurological diseases.

BRL 55834 is an orally and potent potassium channel activator. BRL 55834 exhibits great bronchodilator potency but reduces tendency to lower arterial blood pressure. BRL 55834 has the potential to use as a bronchodilator.