| Bioactivity | 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]. |
| Target | IC50: 0.68 μM (hNKCC1A), 4.0 μM (hNKCC2A) |
| Invitro | 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]. Animal Model: |
| Name | Bumetanide |
| CAS | 28395-03-1 |
| Formula | C17H20N2O5S |
| Molar Mass | 364.42 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 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 |
Bumetanide
CAS: 28395-03-1 F: C17H20N2O5S W: 364.42
Bumetanide (Ro 10-6338; PF 1593), a highly potent loop diuretic, is a Na+-K+-Cl+ cotransporter (NKCC) blocker. Bumetanid
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