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504041 CaCC Blocker IV, Benzbromarone - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₁₂Br₂O₃

Products

Catalog NumberPackaging Qty/Pack
5.04041.0001 Glass bottle 100 mg
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
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
Global Trade Item Number
Catalog Number GTIN
5.04041.0001 04055977264234

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
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 Protect from light
-20°C
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.