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

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

Cat. No.: HY-17468 Purity: 99.91%
Handling Instructions

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.

Bumetanide Chemical Structure

Bumetanide Chemical Structure

CAS No. : 28395-03-1

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Based on 2 publication(s) in Google Scholar

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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 IC 50 value of 0.54 μM[2].

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-life of 21.4 min, 53.8 min and 137 min for 2 mg/kg, 8 mg/kg and 20 mg/kg, respectively, in rats[4].

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

Animal Model: Normotensive Sprague-Dawley rats (250 to 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
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 )
Clinical Trial
Molecular Weight

364.42

Formula

C₁₇H₂₀N₂O₅S

CAS No.

28395-03-1

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, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (274.41 mM)

H2O : 0.1 mg/mL (0.27 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2744 mL 1.3720 mL 2.7441 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.91%

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Keywords:

BumetanideRo 10-6338 PF 1593PF1593PF 1593PF-1593NKCCNa-K-Cl cotransporterNa(+)-K(+)-Cl(-) cotransporterNa+-K+-Cl− cotransporterneonatalseizuresdiureticNa(+)-K(+)-Cl(+)cotransporterNKCC1NKCC2MCAOmiddlecerebralarteryocclusionInhibitorinhibitorinhibit

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