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Submit ReviewDREADD agonist 21
说明： Potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
别名： Compound 21,C21
化学名： 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
纯度： ≥98% (HPLC)
生物活性 for DREADD agonist 21
DREADD agonist 21 is a potent muscarinic DREADD agonist (pEC50 values are 8.91, 8.48 and 7.77 for hM1Dq, hM3Dq and hM4Di in vitro, respectively). Exhibits > 10-fold higher affinity for hM1Dq and hM4Di compared to wild type receptors. Also displays little to no activity at wild type M3 receptors. Activates neurons expressing hM3Dq DREADDS and inhibits activity in neurons expressing hM4Di in vivo. Displays excellent brain permeability. Water soluble salt also available, DREADD agonist 21 hydrochloride (Cat. No. 6422).
技术数据 for DREADD agonist 21
| 分子量 | 278.35 |
| 公式 | C17H18N4 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 56296-18-5 |
| PubChem ID | 11818276 |
| InChI Key | JCBYXNSOLUVGTF-UHFFFAOYSA-N |
| Smiles | C1(N4CCNCC4)=NC(C=CC=C3)=C3NC2=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 DREADD agonist 21
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 27.84 | 100 | |
| ethanol | 27.84 | 100 |
制备储备液 for DREADD agonist 21
以下数据基于产品分子量 278.35。 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 | 3.59 mL | 17.96 mL | 35.93 mL |
| 5 mM | 0.72 mL | 3.59 mL | 7.19 mL |
| 10 mM | 0.36 mL | 1.8 mL | 3.59 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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产品说明书 for DREADD agonist 21
参考文献 for DREADD agonist 21
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. 18 476 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 DREADD agonist 21, please let us know.
关键词: DREADD agonist 21, DREADD agonist 21 supplier, designer, receptors, drugs, DREADDs, hM3Dq, muscarinic, compound, 21, C21, Compound, Non-selective, Muscarinics, 5548, Tocris Bioscience
5 篇 DREADD agonist 21 的引用文献
引用文献是使用了 Tocris 产品的出版物。 DREADD agonist 21 的部分引用包括：
James P et al (2020) Chronic postnatal chemogenetic activation of forebrain excitatory neurons evokes persistent changes in mood behavior. Elife 9 PMID: 32955432
Nathaniel et al (2020) Amygdala inhibitory neurons as loci for translation in emotional memories. Nature 586 407-411 PMID: 33029009
Smith et al (2016) DREADDS: Use and application in behavioral neuroscience. Behav Neurosci 130 137 PMID: 26913540
Peng et al (2023) Highly synchronized cortical circuit dynamics mediate spontaneous pain in mice. J Clin Invest 133 PMID: 36602876
Streamson et al (2023) The gut signals to AGRP-expressing cells of the pituitary to control glucose homeostasis. J Clin Invest 133 PMID: 36787185
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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.