katp channel

U-89232 is an opener of the cardioselective KATP channel.

Glibornuride, a blocker of ATP-sensitive K+ channels (pKi: 5.75), inhibits high-affinity [3H]-glibenclamide binding with potencies corresponding to its K+ channel activity.

KRN 4884 is an opener of the K+ channel. KRN 4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM), in the presence of intracellular ATP (1 mM).

Tifenazoxide is an effective and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.

Aprikalim (RP 52891) is an adenosine triphosphate potassium channel (KATP) opener that protects against nerve damage in a rabbit model of spinal cord ischemia.Aprikalim inhibits vasoconstriction and inhibits the elevation of [Ca2+]i during myocardial paralysis, and can be used to study cardiovascular disease.

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Amiodarone hydrochloride is an anti-anginal agent and a class III antiarrhythmic drug that inhibits potassium channels (including wild-type hERG channels and their tail currents, with an IC₅₀ of approximately 45 nM) as well as voltage-gated sodium channels. This leads to prolonged action potential duration in ventricular and atrial myocytes, resulting in reduced heart rate and vascular resistance. It activates ERK1/2 and p38 MAPK signaling pathways in fibroblasts, promoting cell proliferation and myofibroblast differentiation. Amiodarone hydrochloride is widely used in the study of supraventricular and ventricular arrhythmias and can also be used to establish pulmonary fibrosis animal models.

Hydroxyhexamide ((±)-Hydroxyhexamid) is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agent.

Y-26763 is a K+ channel opener and active metabolite of Y-27152. This is an ATP-sensitive K+ (KATP) channel activator.

Y-27152 is a prodrug of the KATP (Kir6) channel opener Y-26763 and is a long-acting K+ channel opener.

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

Aekatperone, a reversible KATP channel inhibitor, exhibits an IC50 of 9 μM. It is utilized in research related to congenital hyperinsulinism (CHI).

BMS-191095 hydrochloride is a mitochondrial KATP channel opener. It offers cardioprotective benefits without causing vasodilation or impacting electrophysiology. Its protective mechanisms include prolonging myocardial contraction during ischemia, enhancing contractile function post-reperfusion, and reducing lactate dehydrogenase (LDH) release.

Mitiglinide (KAD-1229) is an insulinotropic agent that is an ATP-sensitive K + (K ATP ) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K ATP channel). Mitiglinide is able to be used for the research of type 2 diabetes [1] [2].

Kir6 (KATP) channel antagonist

Iptakalim, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist. Iptakalim is also a K(ir) 6.1/SUR2B activator that can attenuate hypoxia-induced pulmonary arterial hypertension in rats by endothelial function protection.

5-Hydroxydecanoic acid is a selective ATP-sensitive K+ (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoic acid is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.

5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker with an IC50 of approximately 30 μM and a substrate for mitochondrial outer membrane acyl-CoA synthetase, possessing antioxidant properties.

Englitazone sodium is an antidiabetic agent and a novel NSCA and KATP channel blocker.

Non-hydrolyzable AMP analog. Kir6 (KATP) channel blocker. Inhibits fast axonal transport and stabilizes the interaction of membranous organelles with microtubules. Brady (1985) A novel brain ATPase with properties expected for the fast axonal transport motor. Nature 317 73 PMID:2412134 |Yount et al (1971) Adenylyl imidodiphosphate, an adenosine triphosphate analog containing a P-N-P linkage. Biochemistry 10 2484 PMID:4326768 |Hehl and Neumcke (1994) KATP channels of mouse skeletal muscle: mechanism of channel blockage by AMP-PNP. Eur.Biophys.J. 23 231 PMID:7805625

Bepridil hydrochloride (CERM 1978) is a calcium channel blocker that also inhibits Na+/Ca2+ exchange (NCX), sodium channels, and cardiac sarcolemmal KATP channels.

Cibenzoline is an antiarrhythmic agent that inhibits the KATP channel by directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline shows little anticholinergic activity. Cibenzoline markedly reduces LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for hypertrophic obstructive cardiomyopathy research[1][2].

Clamikalant sodium (HMR 1098) is an ATP-dependent potassium channel (KATP) cardiac-selective blocker, used in the study of arrhythmias.

Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable derivative of glutamate, stimulates glucose-induced insulin release, suppresses K_ATP channel activities, inhibits E. gracilis growth, and causes abnormal cell division. This compound is utilized in diabetes research, focusing on glucose transport, phosphorylation, and metabolism.