Bumetanide


CAS No. : 28395-03-1

(Synonyms: Ro 10-6338; PF 1593)

28395-03-1
Price and Availability of CAS No. : 28395-03-1
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Cat. No. : HY-17468
M.Wt: 364.42
Formula: C17H20N2O5S
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic);H2O : < 0.1 mg/mL (ultrasonic)
Introduction of 28395-03-1 :

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 μM and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1][2]. IC50 & Target: IC50: 0.68 μM (hNKCC1A), 4.0 μM (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 μM; 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 IC50 value of 0.54 μM[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-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].

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