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Submit ReviewYIL 781 hydrochloride
说明： Ghrelin receptor (GHS-R1a) antagonist
化学名： 6-(4-Fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone hydrochloride
纯度： ≥98% (HPLC)
生物活性 for YIL 781 hydrochloride
YIL 781 hydrochloride is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo.
化合物库 for YIL 781 hydrochloride
YIL 781 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for YIL 781 hydrochloride
| 分子量 | 445.96 |
| 公式 | C24H28FN3O2.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1640226-17-0 |
| PubChem ID | 74889155 |
| InChI Key | QQGRMONBDBMLSP-FERBBOLQSA-N |
| Smiles | O=C2C1=CC(OC4=CC=C(F)C=C4)=CC=C1N=C(C)N2C[C@@H]3CN(C(C)C)CCC3.Cl |
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 YIL 781 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.6 | 100 | |
| water | 44.6 | 100 |
制备储备液 for YIL 781 hydrochloride
以下数据基于产品分子量 445.96。 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 |
|---|---|---|---|
| 1 mM | 2.24 mL | 11.21 mL | 22.42 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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产品说明书 for YIL 781 hydrochloride
参考文献 for YIL 781 hydrochloride
参考文献是支持产品生物活性的出版物。
Esler et al (2007) Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology 148 5175 PMID: 17656463
Moran and Dailey (2009) Gut peptides: targets for antiobesity drug development? Endocrinology 150 2526 PMID: 19372201
If you know of a relevant reference for YIL 781 hydrochloride, please let us know.
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关键词: YIL 781 hydrochloride, YIL 781 hydrochloride supplier, YIL781, YIL, 781, hydrochloride, HCl, ghrelin, receptors, antagonists, GHS-R1a, GHSR, Ghrelin, Receptors, 3959, Tocris Bioscience
4 篇 YIL 781 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 YIL 781 hydrochloride 的部分引用包括：
Tóth et al (2018) Ghrelin receptor antagonism of hyperlocomotion in cocaine-sensitized mice requires βarrestin-2. Synapse 72 PMID: 28941296
Song et al (2013) Ghrelin modulates lateral amygdala neuronal firing and blocks acquisition for conditioned taste aversion. PLoS One 8 e65422 PMID: 23762368
Marc G et al (2019) Encoding the β-Arrestin Trafficking Fate of Ghrelin Receptor GHSR1a: C-Tail-Independent Molecular Determinants in GPCRs. ACS Pharmacol Transl Sci 2 230-246 PMID: 32259059
Evron et al (2014) G Protein and β-arrestin signaling bias at the ghrelin receptor. J Biol Chem 289 33442 PMID: 25261469
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.