Bumetanide

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].

Product Specifications

CAS Number

[28395-03-1]

Product Name Alternative

Ro 10-6338; PF 1593

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

NKCC

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/bumetanide.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H20N2O5S

Molecular Weight

364.42

Precautions

H315, H319, H335

References & Citations

[1]Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59:42-9.|[2]Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124 (Pt 5) :789-800.|[3]Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24 (9) :1046-56.|[4]S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22 (1) :1-17.6