Potassium Channel Activator

Uridine 5'-monophosphate-¹³C₉,¹⁵N₂ (5'- Uridylic acid-¹³C₉,¹⁵N₂) dilithium is ¹³C and 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.

C3001a is a selective TREK-1 and TREK-2 channel activator with EC₅₀ values of 12.81 μM and 11.31 μM, respectively. C3001a does not affect other two-pore domain K⁺ (K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a can be used for the study of pain and pancreatitis.

Phe-Met-Arg-Phe, amide acetate dose dependently (ED₅₀=23 nM) activates a K⁺ current in the peptidergic caudodorsal neurons.

Diazoxide-d₃ is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.

LQFM020 is an orally active pyrazole derivative. LQFM020 inhibits Ca⁺ and activates K⁺ and NO/cGMP channels to inhibit vasoconstriction. LQFM020 has anti-inflammatory and anti-analgesic activities.

AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC₅₀ values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms.

Bimakalim (EMD-52692) is an ATP-sensitive potassium channel opener. Bimakalim reduces transmural MPO activity. Bimakalim mimics the effects of ischemic preconditioning to reduce infarct size, adenosine release, and neutrophil function in dogs.

Topiramate D12 (Standard) is the analytical standard of Topiramate D12. This product is intended for research and analytical applications. 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.

Flupirtine-d₄ (D 9998-d₄) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine 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.

BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC₅₀ of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model.

Minocycline-d₆ is deuterium 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.

Uridine 5'-monophosphate-¹⁵N₂,d₁₁ (5'- Uridylic acid-¹⁵N₂,d₁₁) dilithium is deuterium and 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.

(S)-(+)-Modafinic acid-d₅ is deuterium labeled (S)-(+)-Modafinic acid.

HUP30 is a vasodilating agent. HUP30 stimulates soluble guanylyl cyclase, activate K⁺ channels, and blocks extracellular Ca²⁺ influx.

Antihypertensive agent 7 is a vasodilator. Antihypertensive agent 7 acts on vascular endothelial cells to activate the PI3K/AKT signaling axis, increase phosphorylated eNOS, release NO, activate the sGC/cGMP pathway in smooth muscle cells, and synergistically activate multiple K⁺ channels in vascular smooth muscle (K_ir/K_v/K_Ca/K_ATP, thereby inducing endothelium-dependent vasodilation. Antihypertensive agent 7 can be used in the research of hypertension.

Uridine 5'-monophosphate-¹³C₉ (5'- Uridylic acid-¹³C₉) dilithium is ¹³C-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.

DABMA is a TMEM175 channel activator with a human EC₅₀ of 17.9 μM. DABMA directly increases TMEM175 channel current via interaction with intracellular, transmembrane, or endosomal lumen-associated domains, and does not alter TMEM175 mRNA or protein levels. DABMA delays endolysosomal substrate degradation, modulates endolysosomal trafficking, increases acidic organelle accumulation, induces cholesterol accumulation and altered late endosome morphology. DABMA can be used for the research of coronavirus disease, Clostridium difficile infection, Pseudomonas aeruginosa infection, rabies, and influenza virus infection.

Pinacidil (Standard) is the analytical standard of Pinacidil. This product is intended for research and analytical applications. Pinacidil is a potent activator of ATP-sensitive potassium channel. Pinacidil is an antihypertensive agent hyperpolarizes vascular smooth muscle by opening K⁺ channels. Pinacidil enhances K⁺-efflux in smooth muscle. Pinacidil has vasorelaxant properties. Pinacidil is able to inhibit spontaneous tone and of reducing agonist induced contractions. Pinacidil can be studied in research area such as cardiovascular diseases.

DCEBIO (Standard) is the analytical standard of DCEBIO (HY-102052). This product is intended for research and analytical applications. DCEBIO is a small/medium conductance calcium-activated potassium (SKCa/IKCa) channel opener and primary neuron signal blocker. It hyperpolarizes the membrane potential of C2C12 myoblasts by activating IKCa channels, thereby promoting myogenic differentiation. The specific biological activity of DCEBIO is manifested in increased myotube formation, enhanced myosin heavy chain II protein levels and myogenin mRNA levels. DCEBIO can be applied in the field of muscle research, especially in muscle-related degenerative diseases such as sarcopenia.

SKA-121 (Standard) is the analytical standard of SKA-121 (HY-107414). This product is intended for research and analytical applications. SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits EC₅₀s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively.