2. Membrane Transporter/Ion Channel
  3. NKCC
  4. Bumetanide

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

Cat. No.: HY-17468 Purity: 99.90%
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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.

CAS No. : 28395-03-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
500 mg In-stock
1 g In-stock
5 g In-stock
10 g In-stock
50 g   Get quote  

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Based on 18 publication(s) in Google Scholar

Other Forms of Bumetanide:

Bumetanide Related Antibodies

Top Publications Citing Use of Products

    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.

    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).

    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).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    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.

    Bumetanide Related Antibodies
    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: T1/2 (21.4 min, 53.8 min and 137 min for 2 mg/kg, 8 mg/kg and 20 mg/kg, respectively )
    Molecular Weight

    364.42

    Formula

    C17H20N2O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

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

    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7441 mL 13.7204 mL 27.4409 mL
    5 mM 0.5488 mL 2.7441 mL 5.4882 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

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    In Vivo:

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: 99.91%

    SDS (393 KB)

    COA (252 KB) HNMR (173 KB) LCMS (463 KB)

    Handling Instructions (2659 KB)
    References

    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
    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
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    Bumetanide Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Bumetanide28395-03-1Ro 10-6338 PF 1593PF1593PF 1593PF-1593NKCCNa-K-Cl cotransporterNa(+)-K(+)-Cl(-) cotransporterNa+-K+-Cl− cotransporterneonatalseizuresdiureticNa(+)-K(+)-Cl(+)cotransporterNKCC1NKCC2MCAOmiddlecerebralarteryocclusionInhibitorinhibitorinhibit

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