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Submit ReviewCGP 12177 hydrochloride
Description: β3 partial agonist. β1/β2 antagonist
Chemical Name: 4-[3-[(1,1-Dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one hydrochloride
Biological Activity for CGP 12177 hydrochloride
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 for CGP 12177 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CGP 12177 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 50 |
Preparing Stock Solutions for CGP 12177 hydrochloride
The following data is based on the product molecular weight 315.8. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 6.33 mL | 31.67 mL | 63.33 mL |
| 2.5 mM | 1.27 mL | 6.33 mL | 12.67 mL |
| 5 mM | 0.63 mL | 3.17 mL | 6.33 mL |
| 25 mM | 0.13 mL | 0.63 mL | 1.27 mL |
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Product Datasheets for CGP 12177 hydrochloride
References for CGP 12177 hydrochloride
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
If you know of a relevant reference for CGP 12177 hydrochloride, please let us know.
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6 Citations for CGP 12177 hydrochloride
Citations are publications that use Tocris products. Selected citations for CGP 12177 hydrochloride include:
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
Kilpatrick et al (2019) Complex Formation between VEGFR2 and the β2-Adrenoceptor. Cell Chem Biol PMID: 30956148
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
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
Do you know of a great paper that uses CGP 12177 hydrochloride from Tocris? Please let us know.
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Literature in this Area
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.