Potassium Channel Activator

NS3623 is an activator of human ether-a-go-go-related gene (hERG1/K_V11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.

Uridine 5'-monophosphate-¹³C₉,¹⁵N₂ disodium is the ¹³C and ¹⁵N labeled Uridine 5'-monophosphate disodium salt (HY-W013175). 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.

1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm.

PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability.

OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K⁺ channels and has Ca²⁺-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.

GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel K_ir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of K_ir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, K_ir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome.

Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV).

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

NS19504 is a Ca²⁺-activated K⁺ channel (BK channel, KCa1.1 channel) activator (EC₅₀=11.0 μM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.

Minoxidil (Standard) is the analytical standard of Minoxidil. This product is intended for research and analytical applications. Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM.

DCEBIO is a small/medium conductance calcium-activated potassium (SK_Ca/IK_Ca) channel opener and primary neuron signal blocker. It hyperpolarizes the membrane potential of C2C12 myoblasts by activating IK_Ca 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.

VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC₅₀=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships.

Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (K_ATP) opener, as well as an α₄β₂-containing nicotinic acetylcholine receptor (nAChR) antagonist.

Isopropyl unoprostone (Unoprostone isopropyl ester), an analogue of a prostaglandin metabolite, is a potent large conductance Ca²⁺-activated K⁺ (BK) channels activator. Isopropyl unoprostone has antiglaucoma effects, lowering intraocular pressure (IOP) by increasing aqueous humour outflow. Isopropyl unoprostone can improve retinal sensitivity and the protection of central retinal sensitivity.

Nicorandil-d₄ (SG-75-d₄) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K+ channels and cardiac ATP-sensitive K+ channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.

Diazoxide (Standard) is the analytical standard of Diazoxide. This product is intended for research and analytical applications. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.

Minoxidil-d₁₀ (U10858-d10) is the deuterium labeled Minoxidil. Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM[1][2][3].

HN37 as a potent and chemically stable antiepileptic agent candidate, with an EC₅₀ of 37 nM for KCNQ2. HN37 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Isopimaric acid is a coniferous tree defense compound. Isopimaric acid binds to AKT and inhibits mTOR phosphorylation, thereby regulating the AKT/mTOR pathway. Isopimaric acid inhibits oxidative stress, inflammation, microglial migration, apoptosis, autophagic flux, ornithine decarboxylase activity, breast cancer proliferation and metastasis, and fungal spore germination. Isopimaric acid also induces M2 microglial polarization, mitochondrial damage, ROS accumulation, starvation-induced colon cancer cell apoptosis, and breast cancer cell cycle arrest. Isopimaric acid activates potassium channels, regulates sodium channels and calcium channels, reduces myocardial excitability, and improves arrhythmia. Isopimaric acid acts as an oxidative substrate for CYP6BW1/3, down-regulates PINK1/Parkin, and regulates calcium homeostasis, oxidative phosphorylation, EMT, and the Wnt pathway. Isopimaric acid exhibits activity against drug-resistant Staphylococcus aureus, repels feeding, and promotes the growth of rice seedlings. Isopimaric acid is suitable for research related to epilepsy, tumors, drug-resistant bacterial infections, atrial fibrillation, hypertension, hyperlipidemia, pulmonary tuberculosis, etc.

Hydrochlorothiazid-d₂ is the 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.