CGP 12177 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 |
| 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 |
Preparing Stock Solutions
The following data is based on the product molecular weight 315.8. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.17 mL | 15.83 mL | 31.67 mL |
| 5 mM | 0.63 mL | 3.17 mL | 6.33 mL |
| 10 mM | 0.32 mL | 1.58 mL | 3.17 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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References
References are publications that support the products' biological activity.
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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Keywords: β3-adrenoceptor b3-adrenoceptor b1-adrenoceptor β1-adrenoceptor α1-adrenoceptor beta1-adrenoceptor b2-adrenoceptor β2-adrenoceptor α2-adrenoceptor beta2-adrenoceptor partial agonists β1-Adrenergic beta1-Adrenergic b1-Adrenerg Adrenergic Beta-3 Receptors
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
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
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
Do you know of a great paper that uses CGP 12177 hydrochloride from Tocris? If so please let us know.
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