CGP 12177 hydrochloride

Cat. No. 1134

CGP 12177 hydrochloride C14H21N3O3.HCl [64208-32-8]

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Chemical Name: 4-[3-[(1,1-Dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one hydrochloride

Biological Activity

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

M.Wt:
315.8
Formula:
C14H21N3O3.HCl
Solubility:
Soluble to 50 mM in water
Storage:
Store at RT
CAS No:
64208-32-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Galitzky et al (1998) On the presence of a putative fourth β-adrenoceptor in human adipose tissue. TiPS 19 164. PMID: 9652187.

Preitner et al (1998) Metabolic response to various β-adrenoceptor agonists in β3-adrenoceptor knockout mice: evidence for a new β-adrenergic receptor in brown adipose tissue. Br.J.Pharmacol. 124 1684. PMID: 9756384.

Strosberg and Pietri-Rouxel (1996) Function and regulation of the β3-adrenoceptor. TiPS 17 373. PMID: 8979772.

Staehelin et al (1983) CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells. J.Biol.Chem. 258 3496. PMID: 6131886.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for CGP 12177 hydrochloride include:

Gherbi et al (2015) Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation. FASEB J 29 2859. PMID: 25837585.

Littmann et al (2015) Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands. Proc Natl Acad Sci U S A 355 183. PMID: 26306764.

Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661. PMID: 26030448.

Gherbi et al (2014) Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP. Br J Pharmacol 171 5431. PMID: 25052258.

Suárez et al (2014) Oleoylethanolamide enhances β-adrenergic-mediated thermogenesis and white-to-brown adipocyte phenotype in epididymal white adipose tissue in rat. Dis Model Mech 7 129. PMID: 24159189.

Do you know of a great paper that uses CGP 12177 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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