MedChemExpress - Model Bumetanide sodium - 28434-74-4
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].MCE products for research use only. We do not sell to patients.
Bumetanide sodium
MCE China：Bumetanide sodium
Brand：MedChemExpress (MCE)
Cat. No.HY-17468A
CAS：28434-74-4
Synonyms：Ro 10-6338 sodium; PF 1593 sodium
Storage：Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：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].
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References：
[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: [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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 [Content Brief]
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