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> Bumetanide [28395-03-1]

Bumetanide [28395-03-1]

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Referencia HY-17468-5g

embalaje : 5g

Marca : MedChemExpress

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Descripciòn

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 )
Peso molecular

364.42

Fòrmula

C17H20N2O5S
No. CAS
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light

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

Solvente y solubilidad
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.

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.
Pureza y Documentación
Referencias

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