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5.04041

CaCC Blocker IV, Benzbromarone

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C17H12Br2O3
CAS Number:
3562-84-3
Molecular Weight:
424.08
MDL number:
MFCD00078962
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light
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assay

≥97% (HPLC)

Quality Level

100

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

storage temp.

−20°C

SMILES string

Brc1c(c(cc(c1)C(=O)c2c3c([o]c2CC)cccc3)Br)O

InChI

1S/C17H12Br2O3/c1-2-13-15(10-5-3-4-6-14(10)22-13)16(20)9-7-11(18)17(21)12(19)8-9/h3-8,21H,2H2,1H3

InChI key

WHQCHUCQKNIQEC-UHFFFAOYSA-N

General description

A cell-permeable uricosuric agent that, in addition to itsknown efficacy in gout treatment, acts as a reversible CaCC blocker and isreported to be more potent than NFA and NPPB in suppressing500 nM Ionomycin induced I- influx in TMEM16A-expressing HEK293cells (IC50 = 9.97, 140, and 150 µM, respectively) as well as inblocking voltage-gated Cl- current in TMEM16B-expressing HEK293cells, while exhibiting much reduced potency against ENaC (α, β, and γ) orCFTR. Shown to significantly reduce mucin secretion from NHBE (normal humanbronchial epithelial) and suppress human ASM (airway smooth muscle) contractionupon muscarinic receptor stimulation.

Biochem/physiol Actions

Primary Target
TMEM16A-CaCC
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Toxic (F)

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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