Benzbromarone, CYP2C9 inhibitor (ab145833)

Overview

  • Product name

    Benzbromarone, CYP2C9 inhibitor
  • Description

    Calcium activated chloride channel blocker. Potent CYP2C9 inhibitor.
  • Alternative names

    • (3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-1-benzofuran-3-yl)methanone
    • 3-(3,5-Dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran
    • Acifugan
    • BBR
    • Benzbromaron
    see all
  • Biological description

    TMEM16A/B calcium activated chloride channel (CaCC) blocker. Potent CYP2C9 inhibitor (Ki = 19 nM). Uricosuric agent inhibiting reabsorption of uric acid mediated by the uric acid transporter URAT1 (SLC22A12). Non-competitive xanthine oxidase inhibitor. Used in the treatment of gout until withdrawn because of continuing concerns over hepatotoxicity.

  • Purity

    > 99%
  • CAS Number

    3562-84-3
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (3,5-Dibromo-4-hydroxyphenyl)(2-ethyl-3-benzofuranyl)methanone
  • Molecular weight

    424.08
  • Molecular formula

    C17H12Br2O3
  • Storage instructions

    Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in DMSO to 100 mM and in ethanol to 10 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Toxic, refer to SDS for further information.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • Source

    Synthetic

References

This product has been referenced in:

  • Gallos G  et al. Functional expression of the TMEM16 family of calcium-activated chloride channels in airway smooth muscle. Am J Physiol Lung Cell Mol Physiol 305:L625-34 (2013). Read more (PubMed: 23997176) »
  • Huang F  et al. Calcium-activated chloride channel TMEM16A modulates mucin secretion and airway smooth muscle contraction. Proc Natl Acad Sci U S A 109:16354-9 (2012). Read more (PubMed: 22988107) »
  • McDonald MG & Rettie AE Sequential metabolism and bioactivation of the hepatotoxin benzbromarone: formation of glutathione adducts from a catechol intermediate. Chem Res Toxicol 20:1833-42 (2007). Read more (PubMed: 18020424) »
  • Kaufmann P  et al. Mechanisms of benzarone and benzbromarone-induced hepatic toxicity. Hepatology 41:925-35 (2005). Read more (PubMed: 15799034) »
  • Iwanaga T  et al. Involvement of uric acid transporter in increased renal clearance of the xanthine oxidase inhibitor oxypurinol induced by a uricosuric agent, benzbromarone. Drug Metab Dispos 33:1791-5 (2005). Read more (PubMed: 16135657) »
  • Locuson CW  et al. A new class of CYP2C9 inhibitors: probing 2C9 specificity with high-affinity benzbromarone derivatives. Drug Metab Dispos 31:967-71 (2003). Read more (PubMed: 12814975) »
  • Sinclair DS & Fox IH The pharmacology of hypouricemic effect of benzbromarone. J Rheumatol 2:437-45 (1975). Read more (PubMed: 1206675) »

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