Na-K-Cl cotransporter

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.

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.

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

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.

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.

Furosemide-d5 is a deuterium marker for Furosemide 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.

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].

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

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