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Submit ReviewDeschloroclozapine
说明： High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapidly blood brain barrier penetrant
别名： DCZ
化学名： 11-(4-Methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
纯度： ≥98% (HPLC)
生物活性 for Deschloroclozapine
Deschloroclozapine is a high affinity and highly potent activator of muscarinic DREADDs (Ki values are 6.3 nM for hM3Dq and 4.2 nM for hM4Di, in vitro; EC50 values are 0.13 nM for hM3Dq and 0.081 nM for hM4Di, in vitro). Derivative of clozapine (Cat. No. 0444). Exhibits 100-fold greater affinity for hM3Dq and hM4Di compared to clozapine N-oxide (CNO; Cat. No. 4936), and 50-fold greater affinity compared to DREADD agonist 21 (Cat. No. 5548). Displays low 'off-target' receptor binding (Ki >100 nM at majority of GPCRs, ion channels and transporters tested). Displays rapid (approx. 10 minutes after i.p injection) binding and activation of hM3Dq and hM4Di in mice and non-human primates. Induces spatial memory deficits in non-human primates expressing hM4Di in the prefrontal cortex.
技术数据 for Deschloroclozapine
| 分子量 | 292.39 |
| 公式 | C18H20N4 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1977-07-7 |
| PubChem ID | 16103 |
| InChI Key | VQHITFFJBFOMBG-UHFFFAOYSA-N |
| Smiles | CN1CCN(C2=NC3=C(C=CC=C3)NC4=CC=CC=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 Deschloroclozapine
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 29.24 | 100 | |
| ethanol | 29.24 | 100 |
制备储备液 for Deschloroclozapine
以下数据基于产品分子量 292.39。 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 |
|---|---|---|---|
| 1 mM | 3.42 mL | 17.1 mL | 34.2 mL |
| 5 mM | 0.68 mL | 3.42 mL | 6.84 mL |
| 10 mM | 0.34 mL | 1.71 mL | 3.42 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
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产品说明书 for Deschloroclozapine
参考文献 for Deschloroclozapine
参考文献是支持产品生物活性的出版物。
Nagai et al (2020) Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys Nat.Neurosci. 23 1157 PMID: 32632286
If you know of a relevant reference for Deschloroclozapine, please let us know.
关键词: Deschloroclozapine, Deschloroclozapine supplier, clozapine, metabolite, clozapine-N-oxide, DREADDs, DREADD, Ligands, muscarnic, receptors, designer, CNO, chemogenetics, DCZ, potent, BBB, brain, blood, barrier, penetrant, Non-selective, Muscarinics, 7193, Tocris Bioscience
1 篇 Deschloroclozapine 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Deschloroclozapine 的部分引用包括：
David E et al (2022) A serotonergic axon-cilium synapse drives nuclear signaling to alter chromatin accessibility. Cell 185 3390-3407.e18 PMID: 36055200
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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.