Bumetanide sodium  (Synonyms: Ro 10-6338 sodium; PF 1593 sodium)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

386.40

C₁₇H₁₉N₂NaO₅S

28434-74-4

O=C(O[Na])C1=CC(NCCCC)=C(OC2=CC=CC=C2)C(S(=O)(N)=O)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]