Art. -Nr.: HY-17468

Bumetanide

(Synonyms: Ro 10-6338; PF 1593)

19 Cited Publications

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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.

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Reinheit: 99.90%
CAS. Nr.: 28395-03-1
Formel: C₁₇H₂₀N₂O₅S
Molecular Weight:364.42

Speicherung:

4°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Bumetanide Chemical Structure

CAS. Nr.: 28395-03-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.68 μM (hNKCC1A), 4.0 μM (hNKCC2A)^[1]

In Vitro

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.

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].

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

Animal Model:

Normotensive Sprague-Dawley rats (250-300 g)^[3]
Dosage:

7.6 mg/kg, 15.2 mg/kg, 30.4 mg/kg
Administration:

Intravenous injection
Result:

Reduced the middle cerebral artery occlusion (MCAO)-induced decrease in ADC values in all four ipsilateral regions (L1-L4).

Animal Model:

Male Sprague-Dawley rats (220-300 g)^[4]
Dosage:

2 mg/kg, 8 mg/kg, 20 mg/kg (Pharmacokinetic Analysis)
Administration:

Intravenous administration
Result:

T_1/2 (21.4 min, 53.8 min and 137 min for 2 mg/kg, 8 mg/kg and 20 mg/kg, respectively )

Chemical Information

CAS. Nr. 28395-03-1
Appearance Solid
Molecular Weight 364.42
Formel C₁₇H₂₀N₂O₅S
Color White to off-white
SMILES

O=C(O)C1=CC(NCCCC)=C(OC2=CC=CC=C2)C(S(=O)(N)=O)=C1
Synonyms

Ro 10-6338; PF 1593
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Publications (19)

All IFBio/Physico-chemical AssayWBIn Vivo Efficacy Study

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Journal Impact Factor

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).
EMBO J

Structural basis for human NKCC1 inhibition by loop diuretic drugs. [Abstract]

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.
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

The apical mucus layer alters the pharmacological properties of the airway epitheliumy. [Abstract]

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, CFTR_inh-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 CFTR_inh-172 (I-172), bumetanide alone (bum) or both compounds together (tot).
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

Activation of TRPM8 promotes K+ secretion in rat epididymal epithelium. [Abstract]

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
Res Sq

2024 Jun 11.
bioRxiv

2024 June 12.
bioRxiv

2024 May 13.
Research Square Preprint

2020 Nov.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7441 mL

13.7204 mL

27.4409 mL

5 mM

0.5488 mL

2.7441 mL

5.4882 mL

10 mM

0.2744 mL

1.3720 mL

2.7441 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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

19 Cited Publications

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Bumetanide

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Publications Citing Use of MedChemExpress (MCE) Bumetanide

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bumetanide

Membrane Transporter/Ion Channel Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

Human Metabolite Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Bumetanide

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bumetanide Related Classifications

HY-17468 Related Classifications