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Submit ReviewCGP 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).
分子量 | 315.8 |
公式 | C14H21N3O3.HCl |
储存 | 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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: CGP 12177 hydrochloride, CGP 12177 hydrochloride supplier, 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, 1134, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CGP 12177 hydrochloride 的部分引用包括:
Kilpatrick et al (2019) Complex Formation between VEGFR2 and the β2-Adrenoceptor. Cell Chem Biol PMID: 30956148
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
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
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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.