504041 CaCC Blocker IV, Benzbromarone - Calbiochem

504041
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₁₂Br₂O₃

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      Glass bottle 100 mg
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      Description
      OverviewA cell-permeable uricosuric agent that, in addition to its known efficacy in gout treatment, acts as a reversible CaCC blocker and is reported to be more potent than NFA (Cat. No. 481987) and NPPB (Cat. No. 484100) in suppressing 500 nM Ionomycin- (Cat. Nos. 407950, 407952, and 407953) induced I- influx in TMEM16A-expressing HEK293 cells (IC50 = 9.97, 140, and 150 µM, respectively) as well as in blocking voltage-gated Cl- current in TMEM16B-expressing HEK293 cells, while exhibiting much reduced potency against ENaC (α, β, and γ) or CFTR. Shown to significantly reduce mucin secretion from NHBE (normal human bronchial epithelial) and suppress human ASM (airway smooth muscle) contraction upon muscarinic receptor stimulation.
      Catalogue Number504041
      Brand Family Calbiochem®
      Synonyms(3,5-dibromo-4-hydroxyphenyl)(2-ethylbenzofuran-3-yl)methanone, ANO Blocker IV, Anoctamin Blocker IV, BBR, CaCC Blocker IV, Calcium-Activated Chloride Channel Blocker IV, TMEM16 Blocker IV
      References
      ReferencesKobayashi, K., et al. 2012. Drug Metab. Pharmacokinet. In press.
      Zhang, C.H., et al. 2013. Am. J. Respir. Crit. Care Med. 187, 374.
      Huang, F., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 16354.
      Fujimori, S., et al. 2011. Nucleosides Nucleotides Nucleic Acids 30, 1035.
      Perez-Ruiz, F., et al. 1998. Ann. Rheum. Dis. 57, 545.
      Product Information
      FormWhite powder
      Hill FormulaC₁₇H₁₂Br₂O₃
      Chemical formulaC₁₇H₁₂Br₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTMEM16A-CaCC
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 25

      Toxic if swallowed.
      S PhraseS: 45

      In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Toxic
      Hazardous Materials Attention: Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      CaCC Blocker IV, Benzbromarone - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      CaCC Blocker IV, Benzbromarone - Calbiochem Certificates of Analysis

      TitleLot Number
      504041

      References

      Reference overview
      Kobayashi, K., et al. 2012. Drug Metab. Pharmacokinet. In press.
      Zhang, C.H., et al. 2013. Am. J. Respir. Crit. Care Med. 187, 374.
      Huang, F., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 16354.
      Fujimori, S., et al. 2011. Nucleosides Nucleotides Nucleic Acids 30, 1035.
      Perez-Ruiz, F., et al. 1998. Ann. Rheum. Dis. 57, 545.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision23-May-2013 JSW
      Synonyms(3,5-dibromo-4-hydroxyphenyl)(2-ethylbenzofuran-3-yl)methanone, ANO Blocker IV, Anoctamin Blocker IV, BBR, CaCC Blocker IV, Calcium-Activated Chloride Channel Blocker IV, TMEM16 Blocker IV
      DescriptionA cell-permeable uricosuric agent that, in addition to its known efficacy in gout treatment, acts as a reversible CaCC blocker and is reported to be more potent than NFA (Cat. No. 481987) and NPPB (Cat. No. 484100) in suppressing 500 nM Ionomycin- (Cat. Nos. 407950, 407952, and 407953) induced I- influx in TMEM16A-expressing HEK293 cells (IC50 = 9.97, 140, and 150 µM, respectively) as well as in blocking voltage-gated Cl- current in TMEM16B-expressing HEK293 (64% inhibition with 10 µM BBR vs. 47% inhibition with 300 µM NFA; by whole cell patch clamp), while exhibiting much reduced potency against voltage-gated current via ENaC (α, β, and γ) or CFTR (by 25% and 17% with 10 µM BBR, respectively, using HEK293 ENaC or CFTR transfectants). Shown to significantly reduce 100 µM ATP-induced CaCC current (IAC current = 1.137 vs. 3.099 µA/cm2 with or without 10 µM BBR) and mucin secretion from NHBE (normal human bronchial epithelial) as well as suppress human ASM (airway smooth muscle) contraction upon muscarinic receptor stimulation.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₂Br₂O₃
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Toxic
      ReferencesKobayashi, K., et al. 2012. Drug Metab. Pharmacokinet. In press.
      Zhang, C.H., et al. 2013. Am. J. Respir. Crit. Care Med. 187, 374.
      Huang, F., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 16354.
      Fujimori, S., et al. 2011. Nucleosides Nucleotides Nucleic Acids 30, 1035.
      Perez-Ruiz, F., et al. 1998. Ann. Rheum. Dis. 57, 545.