atp-sensitive

1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one is an isomer of Rilmakalim, a potassium channel opener (PCO), which can activate ATP-sensitive K+ channels in the heart or other tissues

PCO 400 is an analog of comakalim that acts as a selective and potent ATP-sensitive K+ channel opener.

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.

Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma

5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker with IC50 of about 30 μM. 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase with antioxidant property.

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.

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)1299-1304(2001) 3.Yamada, M., Isomoto, S., Matsumoto, S., et al.Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K+ channelJ. Physiol.499(Pt 3)715-720(1997)

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

ZM 226600 is an ATP-sensitive potassium channel opener with an EC50 value of 500 nM. ZM226600 has an inhibitory effect on spontaneous bladder activity.

Foslevcromakalim (QLS-101), an ATP-sensitive potassium channel opener, serves as a proagent for ocular hypotensive effects [1] [2].

Kaurenoic acid (kaurenoate) has anti-inflammatory potential in acetic acid-induced colitis, decreases in MDA level. Kaurenoic acid exerts a uterine relaxant effect acting principally through calcium blockade and in part, by the opening of ATP-sensitive potassium channels. Kaurenoic acid exhibits an analgesic effect in a consistent manner and that its mechanisms involve the inhibition of cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. Kaurenoic acid derivatives have an antimicrobial activity of substituted on carbon-15 at concentrations greater than or equal to 250 μg/ml. Kaurenoic acid has inhibitory effects on the LPS-induced inflammatory response in RAW264.7 macrophages.

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877).

Linogliride fumarate is the fumarate salt of Linogliride. Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

Clamikalant inhibits ATP-sensitive potassium channel.

U-56324 is a hypoglycemic agent derived from nicotinic acid. It was found to inhibit the activity of ATP-sensitive potassium channels in excised patches from mouse pancreatic B-cells.

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.

Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is formed by the CYP3A isozyme. Amiodarone is an antiarrhythmic drug that inhibits ATP-sensitive potassium channels with an IC50 of 19.1 μM. It is the main active metabolite of amiodaro

AZ-DF 265 is a hypoglycaemic drug which stimulates insulin release. AZ-DF-265 inhibits ATP-sensitive potassium channels and displaces [3H]-glibenclamide from the sulphonylurea receptor.

Paederosidic acid methyl ester has antinociception, is possibly related to the pathway of NO-cGMP-ATP sensitive K(+) channels.

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

Clamikalant sodium is a non-selective, ATP-sensitive potassium (KATP) channel blocker that can be used to study cardiac arrhythmias.

MCC-134 is an inverse agonist for the pancreatic-type ATP-sensitive K(+) channel. It also used as a vascular relaxing agent.

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg/kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

Nicorandil N-oxide, a metabolite of nicorandil, functions as an activator of the ATP-sensitive potassium channel Kir6.2 (SUR2B/Kir6.2) and is associated with the sulfonylurea receptor 2B (SUR2B), while also serving as a nitric oxide donor.

P-1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species causing cardioprotection of rabbit hearts. P-1075 is an effective activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) (EC50: 45 nM fo

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

BMS 180448 is a prototype mitochondrial ATP-sensitive K+ (Mitok (ATP)) channel opener with cardioprotective and vasodilating properties.

Glibornuride is an ATP-sensitive K+ channels (KATP channel) blocker ( pKi: 5.75). It is an antidiabetic agent.

Tilisolol is a nonselective blocker of beta-adrenergic. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs.

Way 120491 activates ATP-sensitive potassium channels.

Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM). Atpenin A5 is also an effective mKATP channel agonist and cardioprotective agent[1].

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].

Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABAA receptors and to antioxidant properties.Isopulegol presents significant gastroprotective effects in both ethanol- and indomethacin-induced ulcer models, which appear to be mediated, at least in part, by endogenous prostaglandins, K(ATP) channel opening, and antioxidant properties.

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5 mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

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

Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

ZM-181037 is an ATP-sensitive potassium channel-blocker and a eukalemic diuretic.

BMS-191095 is mitochondrial ATP-sensitive potassium (mitoKATP) channel activator.

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.