katp

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

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.OR-1896 can be used to study heart failure and vascular dysfunction. OR-1896 can be used to study heart failure and vascular dysfunction.

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.

Minoxidil (U10858) is an orally administered vasodilator with hair growth stimulatory and antihypertensive effects.

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.

Mitiglinide calcium hydrate (S-21403 calcium hydrate) is a drug for the treatment of type 2 diabetes. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells. Mitiglinide belongs to the meglitinide class of blood glucose-lowering drugs and is currently co-marketed in Japan by Kissei and Takeda.

Glipizide (CP 28720) is a short-acting, second-generation sulfonylurea with hypoglycemic activity.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

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

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.

Polydatin (Piceid), the glycoside of Resveratrol, is originally isolated from the Chinese herb Polygonum cuspidatum. The compound can inhibit platelet aggregation and elevate the ratios of LDL-C HDL-C and TC HDL-C. In the myocardial cell, white blood cell, vascular smooth muscle cell, and endothelial cell, Polydatin can inhibit ICAM-1 expression, elevate Ca2+, weaken white blood cell-endothelial cell adhesion, and activate KATP channels.

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

Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.

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

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).

Naminidil is an opener of cyanoguanidine KATP.

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.

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.

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].