Benzbromarone

SKU: orb1225213

Description

A uricosuric agent and non-competitive inhibitor of xanthine oxidase (Ki=8.5 uM); also has potentcy for CYP2C9; also blocks calcium-activated chloride channel (CaCC) TMEM16A with IC50 of 9.97 uM in HEK293 cells.Other Indication Withdrawn.

Key Properties

• CAS Number: 3562-84-3
• MW: 424.0834
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂Br₂O₃
• SMILES: O=C(C1=CC(Br)=C(O)C(Br)=C1)C2=C(CC)OC3=CC=CC=C23
• Target: Xanthine Oxidase (XAO)
• Solubility: DMSO: ≥ 39 mg/mL

Bioactivity

• In Vivo:
  Animal model: High fat diet (HFD)-induced obese (DIO) mice. Dosage: 25 mg/kg, 50 mg/kg. Administration: Intragastric (i. g.). Result: Aggravated lipid accumulation in the liver of DIO mice. Significantly increased triglyceride accumulation and AST, ALT levels. Regulated multiple lipid metabolism genes and the expression of protein markers associated with apoptosis, endoplasmic reticulum stress, and inflammation in the liver of DIO mice. Animal model: Cisplatin treated rats. Dosage: 10 mg/kg. Administration: Oral gavage (p.o.). Result: Ameliorated the elevation in serum creatinine and blood urea nitrogen (BUN) levels induced by cisplatin. Counteracted oxidative stress induced by cisplatin and enhances anti-oxidant defenses in kidney. Alleviated the inflammatory events of nephrotoxicity induced by cisplatin.
• In Vitro:
  Cell Cytotoxicity Assay Cell line: HBMVECs. Concentration: 5 μM, 10 μM, 20 μM. Incubation time: 24 h. Result: Improved the viability reduced by propofol. Western blot analysis. Cell line: HepG2 cells. Concentration: 1 μM, 2 μM, 5 μM, 10 μM, 20 μM, 50 μM, 100 μM. Incubation time: 2 h, 6 h, 24 h. Result: Increased NRF2 protein expression in HepG2 cells exposed for 2 h, 6 h and 24 h at any concentration. Significantly accumulated the protein of NRF2 in the nuclear fraction after exposure to 100 μM at any time point. Caused an increase in the protein expression of TRX1 and TRX2.Significantly increased the ratio of oxidized TRX2 to reduced TRX2 at a concentration of 100 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MJ10061 | NSC 85433

Quick Database Links

Gene Symbol

Xanthine Oxidase (XAO)