na-k-cl cotransporter

Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.

Torsemide (AC-4464) is an anilinopyridine sulfonylurea belonging to the class of loop diuretics. Torsemide has a prolonged duration of action compared to other loop diuretics, is extensively protein bound in plasma and has a relatively long half-life.

Azosemide is a potent NKCC1 inhibitor (IC50s: 0.246 µM and 0.197 µM for hNKCC1A and NKCC1B).

Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used for edema and chronic renal insufficiency.

ZT-1a is a SPAK inhibitor.ZT-1a inhibits SPAK.ZT-1a can be used for the prevention and treatment of neurodegenerative and neurocognitive disorders.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Bumetanide (Standard) is the standard substance of Bumetanide, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.

Bumetanide-D5 is a deuterium-labeled Bumetanide. Bumetanide (T0108) is a Na+-K+-Cl- (NKCC1) inhibitor (IC50s: 0.68 and 4.0 μM for hNKCC1A and hNKCC2A).

Piretanide, an orally active loop diuretic, is recognized as a relatively safe and effective pharmacological agent with notable diuretic capacity. Piretanide exhibits potential for research in the treatment of congestive heart failure, with a distinct advantage due to its potassium-sparing properties that may reduce electrolyte imbalance. Piretanide can also be applied within experimental frameworks directed at the study of hypertension, further supporting its utility in cardiovascular research models.

Compound 2, known as KCC2 potentiators-1, acts as an enhancer of the potassium chloride cotransporter-2 (KCC2). It holds potential for applications in studies related to neurological disorders.

Carbonic anhydrase inhibitor32 (compound 5B) is an orally active, selective inhibitor of hCA (carbonic anhydrase) II/VII, with Ki values of 6.3 nM for hCA II, 10.1 nM for hCA VII, and 681 nM for hCA I. It shows potential for neuroprotection and anticonvulsant effects by reducing mTOR activation and increasing hippocampal KCC2 levels.

Furosemide sodium (Frusemide Sodium) is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.

Bumetanide sodium is a potent loop diuretic that acts as a blocker for the sodium-potassium-chloride cotransporter (NKCC). It selectively inhibits NKCC1 and NKCC2, with IC50 values of 0.68 μM and 4.0 μM for hNKCC1A and hNKCC2A, respectively [1] [2].

ARN23746 (IAMA-6) is a selective NKCC1 inhibitor with neuroprotective activity, used in the research of brain diseases including drug-resistant epilepsy (such as temporal lobe epilepsy TLE, Dravet syndrome DrS), autism spectrum disorder ASD, and Down syndrome DoS.

Furosemide-D5 is a deuterium marker for Furosemide (T0837) and can be used in isotope tracer experiments.Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC), NKCC1, and NKCC2 cotransporter proteins and GABAA receptor antagonist and is used as diuretic reagent, congestive heart failure, hypertension and edema.

Torsemide (Standard) is the standard substance of Torsemide, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Torsemide (AC-4464) is an anilinopyridine sulfonylurea belonging to the class of loop diuretics. Torsemide has a prolonged duration of action compared to other loop diuretics, is extensively protein bound in plasma and has a relatively long half-life.

CAII/VII-IN-1 is an orally active inhibitor of hCA II (KI= 12.3 nM) and hCA VII (KI= 22.6 nM), showing no significant activity towards hCA I. In vivo, it demonstrates excellent neuroprotective properties in a Pilocarpine-induced epilepsy model. It upregulates KCC2 and inhibits mTOR, contributing to its neuroprotective effects. CAII/VII-IN-1 exhibits no significant neurotoxicity or changes in liver and kidney function, making it a useful compound for epilepsy research.

CAII-IN-12 (compound 6c) is a potent and selective inhibitor of carbonic anhydrase (CA) II and VII, with inhibition constants hCA II Ki= 47.8 nM and hCA VII Ki= 3.6 nM, and exhibits antiepileptic activity. It is selective for hCA I with a Ki of 370 nM. In mouse models of epilepsy induced by Pentylenetetrazol and Pilocarpine, CAII-IN-12 demonstrates strong anticonvulsant effects. Additionally, it increases the expression of KCC2 in the hippocampus, maintains neuronal integrity, and reduces mTOR activity. CAII-IN-12 is applicable for epilepsy research.