Potassium Channel Activator

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC₅₀ values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with K_i values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons.

NIP-121 is a new type of potassium channel opener. NIP-121 significantly reduces mean pulmonary artery pressure and total pulmonary resistance through vasodilation. NIP-121 can be used for research on pulmonary arterial hypertension.

YM 934 is a potassium channel opener. YM 934 inhibits neurogenic plasma leakage. YM 934 inhibits airway neurogenic inflammation.

12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca²⁺-activated K⁺ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABA_A antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca²⁺ and stimulates transmitter release.

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

Siponimod-d₁₁ (BAF-312-d₁₁) is deuterium labeled Siponimod (HY-12355). Siponimod 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 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 can be used in research related to multiple sclerosis.

Kv7.2 activator-1 (Compound 8) is a Kv7.2/3 activator with an EC₅₀ of 178 nM. Kv7.2 activator-1 has a long half-life of 120 minutes in HLM.

Kv7 activator-1 (Page 66) is a Kv7 channel activator. Kv7 activator-1 can be used for the studies of depression disorders, neurodegenerative diseases or pain disorders.

KI 1769 is a potassium channel opener. KI 1769 can exhibit vasodilating effect. KI 1769 prolongs the micturition interval and reduces the resistance to fluid infusion through the urethral lumen. KI 1769 can be used for the research of cardiovascular disease.

PF-05020182 is an orally active opener for Kv7 channel, that activates human Kv7.2/7.3, Kv7.4 and Kv7.3/7.5 with EC₅₀ of 334, 625 and 588 nM, respectively. PF-05020182 exhibits anticonvulsant activity in rats corneal electric shock-induced tonic seizure (MES) models. PF-05020182 is blood-brain barrier (BBB) penetrable.

Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine 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 exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

QO-40, a pyrazolo[1,5-a]pyrimidine-7(4H)-one (PPO) derivative, is a KCNQ2/KCNQ3 K⁺ channels activator with an EC₅₀ of 6.94 μM. QO-40 stimulated Ca²⁺-activated K⁺ current (I_K(Ca)) with an EC₅₀ value of 2.3 μM in pituitary GH3 lactotrophs.

Uridine 5'-monophosphate-¹⁵N₂ (5'- Uridylic acid-¹⁵N₂) dilithium is 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.

AL 0671 is a potassium channel opener. AL 0671 can inhibit nonenzymatic glycation of protein and LDL oxidation. AL 0671 can be used for the researches of cardiovascular and metabolic disease, such as hypertensive diabetes.

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

Docosahexaenoyl glycine is a PUFA analogue. Docosahexaenoyl glycine has activating effects on IKs channels and restore the function of IKs channels with LQT1 mutation.

BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC₅₀ = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K⁺ efflux to hyperpolarize the cell membrane and reducing Ca²⁺ influx. BMS-223131 can be used for the research of neurological disease, such as stroke.

TCV 295 is an orally active potassium channel opener. TCV 295 can reduce blood pressure, systemic vascular resistance and myocardial O2 consumption. TCV 295 can be used for the research of cardiovascular disease, such as hypertension.

JTV-506 is a potent ATP-sensitive potassium channel opener. JTV-506 inhibits Histamine (HY-B1204)-induced contraction of tracheal smooth muscle by activation of K_ATP channels. JTV-506 attenuates pulmonary vascular tone through its direct action on vascular smooth muscle cells. JTV-506 can be used for pulmonary hypertension research.

Rilmakalim (HOE 234) is a potassium channel opener (PCO) that activates ATP-sensitive K⁺ channels in the heart or other tissues.