Bumetanide

28395-03-1

364.42

DMSO : >= 100 mg/mL (274.41 mM); H2O : 0.1 mg/mL (0.27 mM; Need ultrasonic)

Membrane Transporter/Ion Channel

Bumetanide (Ro 10-6338; PF 1593), a highly potent loop diuretic, is a Na⁺-K⁺-Cl⁺ cotransporter (NKCC) blocker. Bumetanide is a selective NKCC1 inhibitor, but also inhibits NKCC2, with IC₅₀s of 0.68 uM and 4.0 uM for hNKCC1A and hNKCC2A, respectively^[1][2]. IC50 & Target: IC50: 0.68 uM (hNKCC1A), 4.0 uM (hNKCC2A)^[1] In Vitro: Bumetanide has inhibitory effects for the two major human splice variants of NKCCs, hNKCC1A and hNKCC2A ^[1].
Bumetanide (0.03-100 uM; 5 minutes) inhibits the ⁸⁶Rb⁺ uptake in NKCC1A-expressing oocytes in a dose-dependent manner^[1].
Bumetanide inhibits NKCC2 isoform B in HEK-293 cells with an IC 50 value of 0.54 uM^[2].
In Vivo: Bumetanide (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 also reduces infarct size^[3].
Bumetanide shows different half-life of 21.4 min, 53.8 min and 137 min for 2 mg/kg, 8 mg/kg and 20 mg/kg, respectively, in rats^[4].