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Deschloroclozapine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Deschloroclozapine图片
CAS NO:1977-07-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议

产品介绍
Deschloroclozapine是有效的,高亲和力的,选择性的,代谢稳定的基于毒蕈碱的DREADDs的激动剂。Deschloroclozapine抑制[3H]苄基喹啉基(QNB)与hM3Dq和hM4Di的结合,Ki值分别为6.3和4.2nM。据报道Deschloroclozapine在小鼠和非人类灵长类动物中都有多种用途。
Cas No.1977-07-7
Canonical SMILESCN1CCN(C2=NC3=CC=CC=C3NC4=CC=CC=C42)CC1
分子式C18H20N4
分子量292.38
溶解度DMSO: 100 mg/mL (342.02 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Deschloroclozapine is a potent, high affinity, selective, metabolically stable agonist of muscarinic-based DREADDs. Deschloroclozapine inhibites [3H]quinuclidinyl benzilate (QNB) binding to hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM. Deschloroclozapine is reported with utility in both mice and non-human primates for a variety of applications[1].

Deschloroclozapine has greater potencies for DREADDs than previous agonists in vitro. Deschloroclozapine is a potent agonist for hM3Dq with an EC50=0.13 nM. Deschloroclozapine is also a potent agonist for hM4Di with an EC50=0.081 nM[1].Deschloroclozapine is a potent and selective agonist for hM3Dq and hM4Di, it does not display significant agonistic activity for any of the 318 tests wild-type GPCRs at<10 nM[1].

Deschloroclozapine (100 μg/kg; i.v.) exhibits good brain concentration profiles and biostability. Pharmacokinetic studies confirmed that Deschloroclozapine is rapidly accumulated in mouse brains and monkey CSF, while its metabolites are negligible[1].Deschloroclozapine (1 μg/kg; i.p.) selectively and rapidly enhances neuronal activity via hM3Dq-DREADD in vivo, Deschloroclozapine can also be utilized for in vivo neuronal silencing by activating hM4Di, an inhibitory DREADD[1].Deschloroclozapine (1-100 μg/kg; i.v.) selectively induces hM3Dq-mediated metabolic activity[1].Deschloroclozapine (100 μg/kg; i.m.) selectively induces behavioral deficits in hM4Di-expressing monkeys[1]. Animal Model: Macaque monkey; 2.8-8.0 kg; age 3-10 years[1]

[1]. Yuji Nagai, et al. Deschloroclozapine: a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys. bioRxiv.