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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 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].
产品描述 | 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]. |
体外活性 | 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 the 86 Rb + uptake in NKCC1A-expressing oocytes in a dose-dependent manner [1]. Bumetanide sodium inhibits NKCC2 isoform B in HEK-293 cells with an IC 50 value of 0.54 μM [2]. |
体内活性 | 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]. |
分子量 | 386.4 |
分子式 | C17H19N2NaO5S |
CAS No. | 28434-74-4 |
存储 | Shipping with blue ice. |
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