504041 CaCC Blocker IV, Benzbromarone - Calbiochem

504041
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₂Br₂O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04041.0001
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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®
          SynonymsCaCC Blocker IV, Calcium-Activated Chloride Channel Blocker IV, TMEM16 Blocker IV, (3,5-dibromo-4-hydroxyphenyl)(2-ethylbenzofuran-3-yl)methanone, ANO Blocker IV, Anoctamin Blocker IV, BBR
          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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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
          SynonymsCaCC Blocker IV, Calcium-Activated Chloride Channel Blocker IV, TMEM16 Blocker IV, (3,5-dibromo-4-hydroxyphenyl)(2-ethylbenzofuran-3-yl)methanone, ANO Blocker IV, Anoctamin Blocker IV, BBR
          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.