Bumetanide sodium, a highly potent loop diuretic, is aNa⁺-K⁺-Cl⁺cotransporter (NKCC)blocker. Bumetanide sodium is a selectiveNKCC1inhibitor, and also inhibits NKCC2, withIC₅₀s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively^[1][2].

Bumetanide sodium has inhibitory effects for the two major human splice variants of NKCCs, hNKCC1A and hNKCC2A^[1].
Bumetanide sodium (0.03-100 μM; 5 minutes) inhibits the⁸⁶Rb⁺uptake in NKCC1A-expressing oocytes in a dose-dependent manner^[1].
Bumetanide sodium inhibits NKCC2 isoform B in HEK-293 cells with an IC₅₀value of 0.54 μM^[2].

Bumetanide sodium (7.6-30.4 mg/kg; i.v.) attenuates the decrease in apparent diffusion coefficients (ADC) ratios for both cortex and striatum (by 40-67%), indicating reduced edema formation^[3].
Bumetanide sodium also reduces infarct size^[3].
Bumetanide sodium shows different half-lives of 21.4 min, 53.8 min and 137 min following 2 mg/kg, 8 mg/kg and 20 mg/kg intravenous injection, respectively, in rats^[4].

386.40

C₁₇H₁₉N₂NaO₅S

28434-74-4

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