CGP 12177 hydrochloride

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Cat.No. 1134 - CGP 12177 hydrochloride | C14H21N3O3.HCl | CAS No. 64208-32-8
Description: β3 partial agonist. β12 antagonist
Chemical Name: 4-[3-[(1,1-Dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one hydrochloride
Datasheet
Citations (5)
Reviews
Literature

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
Storage Store at RT
CAS Number 64208-32-8
PubChem ID 11957517
InChI Key YQVFCYCTITZLSX-UHFFFAOYSA-N
Smiles Cl.CC(C)(C)NCC(O)COC1=CC=CC2=C1NC(=O)N2

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.

Solubility Data

Solubility Soluble to 50 mM in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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

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


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5 Citations for CGP 12177 hydrochloride

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

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

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

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

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


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Literature in this Area

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