Bumetanide sodium 是一种高效的利尿剂，是 Na+-K+-Cl+协同转运蛋白 (NKCC) 的阻断剂。Bumetanide sodium 是选择性的NKCC1抑制剂，但对 NKCC2 也有抑制作用，对 hNKCC1A 和 hNKCC2A 作用的IC50值分别为 0.68 和 4.0 μM。

Bumetanide sodium, a highly potent loop diuretic, is a Na + -K + -Cl + cotransporter (NKCC) blocker. Bumetanide sodium is a selective NKCC1 inhibitor, and also inhibits NKCC2, with IC 50 s 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 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].

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].

28434-74-4

C17H19N2NaO5S

386.4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years