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2-Phenylmelatonin

Cat. No. 0680 3 篇引用文献 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： Potent melatonin agonist
化学名： N-[2-(5-Methoxy-2-phenylindol-3-yl)ethyl]acetamide
纯度： ≥98% (HPLC)
说明书
引用文献 (3)
评论 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for 2-Phenylmelatonin

2-Phenylmelatonin is a highly potent melatonin agonist; displays higher affinity and greater potency than melatonin itself. The EC50 values for G protein activation in MT1 and MT2-transfected cells are 65 and 58 pM respectively.

技术数据 for 2-Phenylmelatonin

分子量 308.38
公式 C19H20N2O2
储存 Desiccate at +4°C
纯度 ≥98% (HPLC)
CAS Number 151889-03-1
PubChem ID 4018512
InChI Key OFCLARYYBGKCHN-UHFFFAOYSA-N
Smiles COC1=CC=C2NC(=C(CCNC(C)=O)C2=C1)C1=CC=CC=C1

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.

溶解性数据 for 2-Phenylmelatonin

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 30.84 100
DMSO 30.84 100

制备储备液 for 2-Phenylmelatonin

以下数据基于产品分子量 308.38。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 3.24 mL 16.21 mL 32.43 mL
5 mM 0.65 mL 3.24 mL 6.49 mL
10 mM 0.32 mL 1.62 mL 3.24 mL
50 mM 0.06 mL 0.32 mL 0.65 mL

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产品说明书 for 2-Phenylmelatonin

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for 2-Phenylmelatonin

参考文献是支持产品生物活性的出版物。

Nonno et al (1998) Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells. Br.J.Pharmacol. 124 485 PMID: 9647472

Nonno et al (1999) Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1-antagonists. Br.J.Pharmacol. 127 1288 PMID: 10455277

Spadoni et al (1993) 2-Substituted 5-methoxy-N-acetyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity. J.Med.Chem. 36 4069 PMID: 8258829

If you know of a relevant reference for 2-Phenylmelatonin, please let us know.

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关键词: 2-Phenylmelatonin, 2-Phenylmelatonin supplier, Potent, melatonin, agonists, MT, Receptors, Melatonin, (MT), 0680, Tocris Bioscience

3 篇 2-Phenylmelatonin 的引用文献

引用文献是使用了 Tocris 产品的出版物。 2-Phenylmelatonin 的部分引用包括：

Stauch et al (2019) Structural basis of ligand recognition at the human MT1 melatonin receptor Nature 569 284 PMID: 31019306

Johansson et al (2019) XFEL structures of the human MT2 melatonin receptor reveal the basis of subtype selectivity. Nature 569 289 PMID: 31019305

Akoume et al (2019) A Differential Hypofunctionality of Gαi Proteins Occurs in Adolescent Idiopathic Scoliosis and Correlates with the Risk of Disease Progression. Sci Rep 9 10074 PMID: 31296888

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2-Phenylmelatonin 的评论

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Highly recommended for in vitro stabilization and crystallization of melatonin receptors.
By Anonymous on 10/11/2022
分析类型： In Vitro
种属： Human

After trying many other melatonin receptor ligands, this has become our gold standard for stabilizing MT1 and MT2 melatonin GPCRs for in vitro studies. Given its high potency, relatively low micromolar concentrations are sufficient to achieve the desired effect. We found that it sufficiently stabilizes MTRs for crystallization purposes. Additionally, in cell based GPCR activity assays, it is able to achieve an efficacy as high as, or higher, than the endogenous ligand melatonin. Highly recommended if you value maximum stabilization and/or efficacy

Dissolves well in DMSO

PMID: 31019306