5.04041

CaCC Blocker IV, Benzbromarone

• Synonym(e): CaCC Blocker IV, Benzbromarone, CaCC 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
• Empirische Formel (Hill-System): C₁₇H₁₂Br₂O₃
• CAS-Nummer: 3562-84-3
• Molekulargewicht: 424.08
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥97% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

A 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.

A 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.

Biochem./physiol. Wirkung

Primary Target
TMEM16A-CaCC

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Toxic (F)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

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.

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 Acids30, 1035.
Perez-Ruiz, F., et al. 1998. Ann. Rheum. Dis.57, 545.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Piktogramme: GHS06
• Signalwort: Danger
• H-Sätze: H301
• P-Sätze: P264 - P270 - P301 + P310 - P405 - P501
• Gefahreneinstufungen: Acute Tox. 3 Oral
• Lagerklassenschlüssel: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable