5.04041
CaCC Blocker IV, Benzbromarone
別名:
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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この商品について
実験式（ヒル表記法）:
C17H12Br2O3
CAS番号:
分子量:
424.08
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
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
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.
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)
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
保管分類
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects