katp channel

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 (Amiodarone HCl) is an antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.

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.

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

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

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.

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.

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

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.

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

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.

Kir6 (KATP) channel antagonist

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

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].

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

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).

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

Levcromakalim (BRL 38227) is an activator of the ATP-sensitive K+ 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.

L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and fatty acid metabolite, accumulates in the sarcolemma and disrupts the membrane lipid environment during ischemia. It inhibits K ATP channel activity by interacting with Kir6.2 without altering single-channel conductance [1].

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.