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Paederosidic acid methyl ester is a ATP‐sensitiveK + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level .
Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877) . Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM .
Glipizide (CP 2872; K 4024) a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2 diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium (KATP) channels among β cells of pancreatic islets of Langerhans .
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 Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation .
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Amiodarone-d10 (hydrochloride) is the deuterium labeled Amiodarone. Amiodarone hydrochloride is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2].
Minoxidil sulfate, a potent and ATP-sensitiveK + channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo .
Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
BMS-191095 is a selective activator of mitochondrial ATP-sensitive potassium (mitoKATP) channels. BMS-191095 inhibits human platelet aggregation by opening mitochondrial K(ATP) channels .
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitivepotassium channel with an IC50 of 19.1 μM .
5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity .
Gliclazide (Standard) is the analytical standard of Gliclazide. This product is intended for research and analytical applications. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitivepotassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
Iptakalim hydrochloride, 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 .
Gliclazide-d4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic[1].
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 .
PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells .
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 .
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitiveK + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus .
Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].
Desethylamiodarone (hydrochloride) (Standard) is the analytical standard of Desethylamiodarone (hydrochloride). This product is intended for research and analytical applications. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitivepotassium channel with an IC50 of 19.1 μM .
Icariside E4 is an antinociceptive agent, and can be isolated from Tabebuia roseo-alba. Icariside E4 has peripheral analgesic activity by ATP-sensitiveK + channel-dependent mechanisms. Icariside E4 also has anti-oxidant, anti-Alzheimer and anti-inflammatory effects .
Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes .
Mitiglinide Calcium (KAD-1229 anhydrous), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide Calcium is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium can be used for the research of type 2 diabetes .
Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes .
Nateglinide-d5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
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].
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels .
Gliclazide-d4 (Standard) is the analytical standard of Gliclazide-d4. This product is intended for research and analytical applications. Gliclazide-d4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic[1].
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[1][2][3].
Glipizide-d11 is the deuterium labeled Glipizide. Glipizide (CP 2872; K 4024) a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2 diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium (KATP) channels among β cells of pancreatic islets of Langerhans[1][2].
Mitiglinide-d5 (calcium) is deuterium labeled Mitiglinide. Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes[1][2].
(2R)-Mitiglinide-d5 (calcium) is deuterium labeled Mitiglinide. Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes[1][2].
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation . P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts .
Mitiglinide-d8 (calcium hydrate) (KAD-1229-d8) is the deuterium labeled Mitiglinide calcium hydrate. Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes[1][2].
Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway .
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway .
Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis .
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitiveP2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
Paederosidic acid methyl ester is a ATP‐sensitiveK + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level .
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 .
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway .
Icariside E4 is an antinociceptive agent, and can be isolated from Tabebuia roseo-alba. Icariside E4 has peripheral analgesic activity by ATP-sensitiveK + channel-dependent mechanisms. Icariside E4 also has anti-oxidant, anti-Alzheimer and anti-inflammatory effects .
The KCNJ10 protein is an inwardly rectifying potassium channel that plays a critical buffering role in potassium in brain glial cells. It facilitates the influx of potassium and is regulated at extracellular levels. KCNJ10 Protein, Rat (Cell-Free, His) is the recombinant rat-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-6*His labeled tag. The total length of KCNJ10 Protein, Rat (Cell-Free, His) is 379 a.a., with molecular weight of 46.6 kDa.
The KCNJ10 protein regulates potassium buffering in brain glial cells, favoring potassium influx due to its inward rectifying properties. Extracellular potassium concentration modulates its voltage dependence, and internal magnesium induces inward rectification by blocking outward current. KCNJ10 Protein, Mouse (Cell-Free, His) is the recombinant mouse-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNJ10 Protein, Mouse (Cell-Free, His) is 379 a.a., with molecular weight of 48.5 kDa.
The KCNJ10 protein is an inwardly rectifying potassium channel that is essential for potassium buffering by glial cells in the brain. It favors potassium influx rather than efflux, and the voltage dependence is regulated by extracellular potassium levels. KCNJ10 Protein, Human (Cell-Free, His) is the recombinant human-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNJ10 Protein, Human (Cell-Free, His) is 379 a.a., with molecular weight of 48.6 kDa.
The KCNJ10 protein is an inwardly rectifying potassium channel that is essential for potassium buffering by glial cells in the brain. It favors potassium influx rather than efflux, and the voltage dependence is regulated by extracellular potassium levels. KCNJ10 Protein, Human (Cell-Free, His, SUMO) is the recombinant human-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-6*His, N-SUMO labeled tag. The total length of KCNJ10 Protein, Human (Cell-Free, His, SUMO) is 379 a.a., with molecular weight of 58.5 kDa.
Amiodarone-d10 (hydrochloride) is the deuterium labeled Amiodarone. Amiodarone hydrochloride is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2].
Gliclazide-d4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic[1].
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].
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].
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[1][2][3].
Glipizide-d11 is the deuterium labeled Glipizide. Glipizide (CP 2872; K 4024) a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2 diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium (KATP) channels among β cells of pancreatic islets of Langerhans[1][2].
Mitiglinide-d5 (calcium) is deuterium labeled Mitiglinide. Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes[1][2].
(2R)-Mitiglinide-d5 (calcium) is deuterium labeled Mitiglinide. Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes[1][2].
Mitiglinide-d8 (calcium hydrate) (KAD-1229-d8) is the deuterium labeled Mitiglinide calcium hydrate. Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes[1][2].
Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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