Bumetanide
Based on 19 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 28395-03-1
- Formula: C17H20N2O5S
- Molecular Weight:364.42
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Storage:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Bumetanide
More- J Neuroinflammation. 2022 Jun 21;19(1):163. [Abstract]
- EMBO J. 2025 Mar;44(5):1540-1562. [Abstract]
- Biochem Pharmacol. 2026 Mar:245:117671. [Abstract]
- Glia. 2024 Dec;72(12):2231-2246. [Abstract]
- Eur J Pharmacol. 2025 Jun 5:996:177447. [Abstract]
- J Physiol. 2025 May;603(9):2619-2632. [Abstract]
- Exp Neurol. 2024 Nov 26:115076. [Abstract]
- iScience. 2026 Jun 3;29(6):115796. [Abstract]
- Cell Calcium. 2026 Mar:134:103117. [Abstract]
- Biomedicines. 2024 Apr 30;12(5):991. [Abstract]
- J Neurotrauma. 2025 May;42(9-10):814-831. [Abstract]
- Viruses. 2026 Mar 12;18(3):350. [Abstract]
- Andrology. 2024 May 22. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- Biochem Biophys Res Commun. 2025 Sep 19:785:152676. [Abstract]
- Res Sq. 2024 Jun 11.
- bioRxiv. 2024 June 12.
- bioRxiv. 2024 May 13.
- Research Square Preprint. 2020 Nov.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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IF
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WB
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In Vivo Efficacy Study
Biological Activity
IC50: 0.68 μM (hNKCC1A), 4.0 μM (hNKCC2A)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Normotensive Sprague-Dawley rats (250-300 g)[3]
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Dosage:7.6 mg/kg, 15.2 mg/kg, 30.4 mg/kg
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Administration:Intravenous injection
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Result:Reduced the middle cerebral artery occlusion (MCAO)-induced decrease in ADC values in all four ipsilateral regions (L1-L4).
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Animal Model:Male Sprague-Dawley rats (220-300 g)[4]
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Dosage:2 mg/kg, 8 mg/kg, 20 mg/kg (Pharmacokinetic Analysis)
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Administration:Intravenous administration
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Result:T1/2 (21.4 min, 53.8 min and 137 min for 2 mg/kg, 8 mg/kg and 20 mg/kg, respectively )
Chemical Information
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CAS No. 28395-03-1
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Appearance Solid
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Molecular Weight 364.42
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Formula C17H20N2O5S
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Color White to off-white
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SMILES
O=C(O)C1=CC(NCCCC)=C(OC2=CC=CC=C2)C(S(=O)(N)=O)=C1
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Synonyms
Ro 10-6338; PF 1593
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (19)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
NLRP3 inflammasome-mediated choroid plexus hypersecretion contributes to hydrocephalus after intraventricular hemorrhage via phosphorylated NKCC1 channels. [Abstract]2022 Jun 21;19(1):163. PMID: 35729645
Bumetanide purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2022 Jun 21;19(1):163. [Abstract]
Representative images of immunofluorescence staining for p-NKCC1 and p-NKCC1-positive cell statistics of the choroid plexus at 3 days following Bumetanide treatment (6 rats/group, Welch's two-tailed unpaired t-test). Bar = 50 μm.
Bumetanide purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2022 Jun 21;19(1):163. [Abstract]
Western blot analysis of p-NKCC1 and NLRP3 in the choroid plexus at 3 days after Bumetanide treatment.
Bumetanide purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2022 Jun 21;19(1):163. [Abstract]
CSF secretion rates after Bumetanide treatment (6-8 rats/group, Welch's two-tailed unpaired t-test).
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EMBO J
2025 Mar;44(5):1540-1562. PMID: 39875725
Bumetanide purchased from MedChemExpress. Usage Cited in: EMBO J. 2025 Mar;44(5):1540-1562. [Abstract]
NKCC1-mediated Cl- influx was inhibited by furosemide, Bumetanide, and torsemide applied externally to the cells at 100 μM concentration.
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Biochem Pharmacol
Sodium-potassium-chloride cotransporter 1 as a novel regulator of DAMPs-mediated alveolar epithelial-macrophage crosstalk in LPS-induced lung inflammation. [Abstract]2026 Mar:245:117671. PMID: 41506546 -
Glia
Endothelin-1 increases Na+-K+-2Cl- cotransporter-1 expression in cultured astrocytes and in traumatic brain injury model: An involvement of HIF1α activation. [Abstract]2024 Dec;72(12):2231-2246. PMID: 39166289 -
Eur J Pharmacol
Loop diuretics mitigate juvenile immobilization treatment-induced hippocampal dysfunction. [Abstract]2025 Jun 5:996:177447. PMID: 40023355 -
J Physiol
2025 May;603(9):2619-2632. PMID: 40047394
Bumetanide purchased from MedChemExpress. Usage Cited in: J Physiol. 2025 May;603(9):2619-2632. [Abstract]
Representative short-circuit current traces (left) and summary graphs (right) from epithelia kept in control conditions, treated with IL-4 or treated with IL-17A/TNF-α. During recordings, CFTRinh-172 (apical, 10 µM) and Bumetanide (basolateral, 100 µM) were added sequentially after stimulation of CFTR with CPT-cAMP. Dotted and dashed lines indicate the baseline for cAMP-activated current and zero current level, as in previous legends. The graphs report the fraction of the cAMP-activated current blocked by CFTRinh-172 (I-172), bumetanide alone (bum) or both compounds together (tot).
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Exp Neurol
Mechanisms of polygalasaponin F against brain ischemia-reperfusion injury by targeting NKCC1. [Abstract]2024 Nov 26:115076. PMID: 39608559 -
iScience
Dim light at night induces cardiac injury in zebrafish embryos via disrupted chloride homeostasis. [Abstract]2026 Jun 3;29(6):115796. PMID: 42291255 -
Cell Calcium
2026 Mar:134:103117. PMID: 41539212 -
Biomedicines
Characterization of a Clinically and Biologically Defined Subgroup of Patients with Autism Spectrum Disorder and Identification of a Tailored Combination Treatment. [Abstract]2024 Apr 30;12(5):991. PMID: 38790952 -
J Neurotrauma
Attenuation of Blood-Brain Barrier Disruption in Traumatic Brain Injury via Inhibition of NKCC1 Cotransporter: Insights into the NF-κB/NLRP3 Signaling Pathway. [Abstract]2025 May;42(9-10):814-831. PMID: 39879999 -
Viruses
Identification of Oncolytic Avian Reovirus Receptors in B16-F10 Cells and the Signaling-Mediated Pathways Involved in Viral Entry. [Abstract]2026 Mar 12;18(3):350. PMID: 41902258 -
Andrology
Cellular mechanism underlying leptin-induced anion secretion of rat epididymal epithelial cells. [Abstract]2024 May 22. PMID: 38778669 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Biochem Biophys Res Commun
Glucose transports in the ileum: mechanism, regulation and physiological role of ileal glucose absorption. [Abstract]2025 Sep 19:785:152676. PMID: 41005286 -
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Solvent & Solubility
DMSO : 100 mg/mL (274.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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;59:42-9. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.7441 mL | 13.7204 mL | 27.4409 mL | 68.6022 mL |
| 5 mM | 0.5488 mL | 2.7441 mL | 5.4882 mL | 13.7204 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7441 mL | 6.8602 mL | |
| 15 mM | 0.1829 mL | 0.9147 mL | 1.8294 mL | 4.5735 mL | |
| 20 mM | 0.1372 mL | 0.6860 mL | 1.3720 mL | 3.4301 mL | |
| 25 mM | 0.1098 mL | 0.5488 mL | 1.0976 mL | 2.7441 mL | |
| 30 mM | 0.0915 mL | 0.4573 mL | 0.9147 mL | 2.2867 mL | |
| 40 mM | 0.0686 mL | 0.3430 mL | 0.6860 mL | 1.7151 mL | |
| 50 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3720 mL | |
| 60 mM | 0.0457 mL | 0.2287 mL | 0.4573 mL | 1.1434 mL | |
| 80 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8575 mL | |
| 100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6860 mL |
Bumetanide Related Classifications
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