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Furosemide NKCC inhibitor

Cat.No.S1603

Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.
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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (199.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 330.74 Formula

C12H11ClN2O5S

Storage (From the date of receipt)
CAS No. 54-31-9 Download SDF Storage of Stock Solutions

Synonyms NSC 269420 SMILES C1=COC(=C1)CNC2=CC(=C(C=C2C(=O)O)S(=O)(=O)N)Cl

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Mechanism of Action

Targets/IC50/Ki
NKCC2
In vitro

Furosemide reversibly alters the responses to tones and clicks of the chinchilla basilar membrane in hair cells, causing response-magnitude reductions that are largest (up to 61 dB, averaging 25-30 dB) at low stimulus intensities at the characteristic frequency (CF) and small or nonexistent at high intensities and at frequencies far removed from CF. This compound also induces response-phase lags that are largest at low stimulus intensities (averaging 77 degrees) and are confined to frequencies close to CF.

This chemical concentration- and time-dependently increases the formation of nitric oxide andprostacyclin. It leads to an enhanced release of kinins into the supernatant of the cells.

It reversibly suppresses low Ca2+-induced epileptiform activity in hippocampus proper and blocks or significantly reduces different types of epileptiform discharges in the low Mg2+ model and the 4-aminopyridine model.

This compound significantly inhibits cell growth in MKN45 cells, but not in MKN28 cells. It diminishes cell growth by delaying the G(1)-S phase progression in poorly differentiated gastric adenocarcinoma cells, which show high expression and activity of NKCC, but not in moderately differentiated gastric adenocarcinoma cells with low expression and NKCC activity.

In vivo

Furosemide (0.25 to 2 mg/kg), administered 4 hours before exercise, reduces right atrial pressure (RAP) and pulmonary arterial pressure (PAP) during exercise in dose-dependent manner in horse.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17052386/
  • [5] https://pubmed.ncbi.nlm.nih.gov/1524299/
  • [6] https://pubmed.ncbi.nlm.nih.gov/22907543/
  • [7] https://pubmed.ncbi.nlm.nih.gov/29915390/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-16)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06941415 RECRUITING
Cirrhosis
Stacy Johnson
2026-06-03 PHASE3
NCT07737964 NOT_YET_RECRUITING
Heart Failure
University Hospital, Montpellier
2026-10 PHASE3
NCT06229990 RECRUITING
Acute Kidney Injury
Chiang Mai University
2024-01-01 PHASE4
NCT07018297 NOT_YET_RECRUITING
Heart Failure; Acute Decompensated Heart Failure
University of Texas Southwestern Medical Center
2026-08 PHASE3
NCT07726134 NOT_YET_RECRUITING
Delayed Graft Function; Kidney Transplantation
London Health Sciences Centre Research Institute OR Lawson Research Institute of St. Joseph's
2026-08
NCT07167862 NOT_YET_RECRUITING
Preeclampsia; Preeclampsia Postpartum; Preeclampsia Severe or Mild
University of California, Irvine
2026-06-15 PHASE4

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