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说明： Potent hM3Dq and hM4Di DREADD agonist in vitro
化学名： 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
纯度： ≥99% (HPLC)
生物活性 for Perlapine
Perlapine is a potent muscarinic DREADD agonist (pEC50 values are 8.38, 8.08 and 7.27 for hM1Dq, hM3Dq and hM4Di in vitro, respectively). Exhibits >10,000-fold selectivity for hM3Dq over hM3 receptors.
技术数据 for Perlapine
| 分子量 | 291.39 |
| 公式 | C19H21N3 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1977-11-3 |
| PubChem ID | 16106 |
| InChI Key | PWRPUAKXMQAFCJ-UHFFFAOYSA-N |
| Smiles | CN(CC4)CCN4C1=NC(C=CC=C3)=C3CC2=C1C=CC=C2 |
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 Perlapine
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 14.57 | 50 | |
| water | 1.46 | 5 温和加热 |
制备储备液 for Perlapine
以下数据基于产品分子量 291.39。 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 | 6.86 mL | 34.32 mL | 68.64 mL |
| 2.5 mM | 1.37 mL | 6.86 mL | 13.73 mL |
| 5 mM | 0.69 mL | 3.43 mL | 6.86 mL |
| 25 mM | 0.14 mL | 0.69 mL | 1.37 mL |
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产品说明书 for Perlapine
参考文献 for Perlapine
参考文献是支持产品生物活性的出版物。
Chen et al (2015) The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem.Neurosci. 6 476 PMID: 25587888
Thompson et al (2018) DREADD agonist 21 (C21) is an effective agonist for muscarinic-based DREADDs in vitro and in vivo. ACS Pharmacol.Transl.Sci. 1 61 PMID: 30868140
If you know of a relevant reference for Perlapine, please let us know.
关键词: Perlapine, Perlapine supplier, Perlapine, potent, selective, hM3Dq, DREADD, agonists, antagonism, designer, receptors, drugs, muscarinic, activators, chemogenetics, DREADDs, Non-selective, Muscarinics, 5549, Tocris Bioscience
1 篇 Perlapine 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Perlapine 的部分引用包括：
Weston et al (2019) Olanzapine: A potent agonist at the hM4D(Gi) DREADD amenable to clinical translation of chemogenetics. Sci Adv. 5 PMID: 31001591
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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。
Chemogenetics Research Bulletin
Produced by Tocris, the chemogenetics research bulletin provides an introduction to chemogenetic methods to manipulate neuronal activity. It outlines the development of RASSLs, DREADDs and PSAMs, and the use of chemogenetic compounds. DREADD ligands and PSEMs available from Tocris are highlighted.
Allosteric GPCR Pharmacology Poster
G protein-coupled receptors (GPCRs) are intrinsically allosteric proteins. This poster provides insights into allosteric mechanisms of GPCR biology, highlighting key facets of GPCR allostery and therapeutic applications of allosteric modulators.
GPCR Efficacy and Biased Agonism Poster
GPCRs can interact with multiple distinct transducers or regulatory proteins and these can be preferentially engaged in an agonist-specific manner giving rise to biased agonism. This poster discusses cutting edge GPCR signaling pharmacology and highlights therapeutic applications of biased agonism.