Product nameBenzbromarone, CYP2C9 inhibitor
DescriptionCalcium activated chloride channel blocker. Potent CYP2C9 inhibitor.
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 Used in the treatment of gout until withdrawn because of continuing concerns over hepatotoxicity.
Storage instructionsStore at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM and in ethanol to 10 mM
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.
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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) »