Bumetanide sodium

CAS: 28434-74-4 F: C17H19N2NaO5S W: 386.40

Bumetanide sodium, a highly potent loop diuretic, is a Na+-K+-Cl+ cotransporter (NKCC) blocker. Bumetanide sodium is a s

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Bioactivity	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 IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1][2].
Invitro	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 86Rb+ uptake in NKCC1A-expressing oocytes in a dose-dependent manner[1].Bumetanide sodium inhibits NKCC2 isoform B in HEK-293 cells with an IC50 value of 0.54 μM[2].
In Vivo	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].
Name	Bumetanide sodium
CAS	28434-74-4
Formula	C17H19N2NaO5S
Molar Mass	386.40
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59: [2]. Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124(Pt 5):789-800. [3]. Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24(9):1046-56. [4]. S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22(1):1-17.6

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