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Submit ReviewJHU 37152
说明： High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
化学名： 8-Chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine
纯度： ≥98% (HPLC)
生物活性 for JHU 37152
JHU 37152 is a high affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.8 nM and 8.7 nM for hM3Dq and hM4Di in vitro, respectively; EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in vitro, respectively). Selectively displaces [3H]clozapine from DREADDs in vivo, but not from other clozapine binding sites. Inhibits locomotor activity in mice expressing hM3Dq and hM4Di in D1-expressing neurons. Brain penetrant in mice, rats and non-human primates.
技术数据 for JHU 37152
| 分子量 | 358.85 |
| 公式 | C19H20ClFN4 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2369979-67-7 |
| PubChem ID | 139033721 |
| InChI Key | NZMZJNNWMSYDNX-UHFFFAOYSA-N |
| Smiles | CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC(F)=C24)CC1 |
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 JHU 37152
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.88 | 100 | |
| ethanol | 35.88 | 100 |
制备储备液 for JHU 37152
以下数据基于产品分子量 358.85。 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 | 2.79 mL | 13.93 mL | 27.87 mL |
| 5 mM | 0.56 mL | 2.79 mL | 5.57 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.79 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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产品说明书 for JHU 37152
参考文献 for JHU 37152
参考文献是支持产品生物活性的出版物。
Bonaventura et al (2019) High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat.Commun. 10 4627 PMID: 31604917
If you know of a relevant reference for JHU 37152, please let us know.
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关键词: JHU 37152, JHU 37152 supplier, JHU37152, DREADD, agonist, agonists, activator, activators, actuator, muscarinic, hM3Dq, hM4Di, brain, penetrant, DREADDs, 7197, Tocris Bioscience
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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.