Darbufelone (mesylate)

• Description :

  Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM) .

• CAS Number :

  [139340-56-0]

• Product Name Alternative :

  CI-1004 (mesylate)

• UNSPSC :

  12352005

• Target :

  Leukotriene Receptor; Prostaglandin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein

• Applications :

  Metabolism-protein/nucleotide metabolism

• Field of Research :

  Inflammation/Immunology; Endocrinology

• Assay Protocol :

  https://www.medchemexpress.com/Darbufelone_(mesylate).html

• Concentration :

  10mM

• Purity :

  99.65

• Solubility :

  DMSO : 110 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

  O=C1N=C(N)S/C1=C\C2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2.CS(=O)(O)=O

• Molecular Formula :

  C19H28N2O5S2

• Molecular Weight :

  428.57

• References & Citations :

  [1]Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry. 2001 Jun 26;40 (25) :7736-45.|[2]Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66 (2) :277-85.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, sealed storage, away from moisture and light)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  FP; LTB4