Furosemide An inhibitor of NKCC and a GABAA receptor antagonist

Furosemide (CAS 54-31-9)

Furosemide | CAS 54-31-9 is rated 5.0 out of 5 by 1.
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Synonym: Frusemide; Lasix; Furanthril; Errolon; Fusid; Fuluvamide; Furanthryl; Furantril; Furosemid
Application: An inhibitor of NKCC and a GABAA receptor antagonist
CAS Number: 54-31-9
Purity: ≥99%
Molecular Weight: 330.74
Molecular Formula: C12H11ClN2O5S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Furosemide is a loop diuretic inhibitor of NKCC (Na+/2Cl-/K+) cotransporter. Furosemide acts as a non-competitive antagonist at GABAA receptors with ~ 100-fold greater selectivity for α6-containing receptors than α1-containing receptors.


References

Thompson et al (1999) Residues in transmembrane domains I and II determine g-aminobutyric acid type AA receptor subtype-selective antagonism by furosemide. Mol.Pharmacol. 55 993. Gutschmidt et al (1999) Anticonvulsant actions of furosemide in vitro. Neuroscience 91 1471.

Physical State :
Solid
Solubility :
Soluble in DMSO (66 mg/ml at 25° C), ethanol (<1 mg/ml at 25° C), water (<1 mg/ml at 25° C), methanol (50 mg/ml), and DMF.
Storage :
Store at room temperature
Melting Point :
220° C (lit.)(dec.)
Boiling Point :
~582.1° C at 760 mmHg (Predicted)
Density :
~1.6 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
11β-HSD1: IC50 = 3.76 µM (human); 11β-HSD1: IC50 = 3.76 µM (mouse); HCO3- stimulated swelling in cat cerebrocortical tissue slice: IC50 = 10 µM; Plasmodium falciparum: IC50 = 12.59 µM; Holo-[acyl-carrieir-protein] synthase: IC50 = 12.7 µM (Bacillus subtilis)
Ki Data :
CA XIV: Ki= 52 nM (human); CA I: Ki= 62 nM (human); CA II: Ki= 65 nM (human); CA VI: Ki= 245 nM (human); CA XII: Ki= 261 nM (human)
pK Values :
pKa: 3.04 (Predicted), pK1: 3.8, pK2: 7.5, pKb: -1.5 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
CB2625000
PubChem CID :
3440
Merck Index :
14: 4309
MDL Number :
MFCD00010549
EC Number :
200-203-6
Beilstein Registry :
840915
SMILES :
NS(=O)(=O)C1=C(Cl)C=C(NCC2=CC=CO2)C(=C1)C(O)=O

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Limmer et al Limmer et al. (PubMed ID 26183401) found that Furosemide increased vasodilator-stimulated phosphoprotein phosphorylation and membrane translocation of NKCC2 via cGkI activation in mice. -SCBT Publication Review
Date published: 2015-03-22
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