CGP 12177 hydrochloride
Chemical Name: 4-[3-[(1,1-Dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one hydrochloride
Biological Activity
CGP 12177 hydrochloride is a partial agonist at β3-adrenoceptors. β1- and β2-adrenoceptor antagonist (Ki values are 0.9, 4 and 88 nM for β1, β2 and β3 receptors respectively).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
On the presence of a putative fourth β-adrenoceptor in human adipose tissue.
Galitzky et al.
TiPS, 1998;19:164 -
Metabolic response to various β-adrenoceptor agonists in β3-adrenoceptor knockout mice: evidence for a new β-adrenergic receptor in brown adipose tissue.
Preitner et al.
Br.J.Pharmacol., 1998;124:1684 -
CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells.
Staehelin et al.
J.Biol.Chem., 1983;258:3496 -
Function and regulation of the β3-adrenoceptor.
Strosberg and Pietri-Rouxel
TiPS, 1996;17:373
Product Datasheets
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Citations for CGP 12177 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for CGP 12177 hydrochloride include:
6 Citations: Showing 1 - 6
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Complex Formation between VEGFR2 and the β2-Adrenoceptor.
Authors: Kilpatrick Et al.
Cell Chem Biol 2019;
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Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
Authors: Littmann Et al.
Proc Natl Acad Sci U S A 2015;355:183
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Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.
Authors: Gherbi Et al.
FASEB J 2015;29:2859
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Application of BRET to monitor ligand binding to GPCRs.
Authors: Stoddart Et al.
Nat Methods 2015;12:661
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Oleoylethanolamide enhances β-adrenergic-mediated thermogenesis and white-to-brown adipocyte phenotype in epididymal white adipose tissue in rat.
Authors: Suárez Et al.
Dis Model Mech 2014;7:129
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Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.
Authors: Gherbi Et al.
Br J Pharmacol 2014;171:5431
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