Bumetanide

• UNSPSC 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].

• Target Antigen:

  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

• 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 Weight:

  364.42

• 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

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Launched

• CAS Number:

  28395-03-1