JHU37152
目录号: PL06868 纯度: ≥98%
CAS No. :2369979-67-7
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中文名称
JHU37152
英文名称
JHU37152
英文别名
JHU37152 (DREADD ligand);JHU37152;s9789;JHU 37152;3-chloro-6-(4-ethylpiperazin-1-yl)-7-fluoro-11H-benzo[b][1,4]benzodiazepine
Cas No.
2369979-67-7
分子式
C19H20ClFN4
分子量
358.84
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
JHU37152 是一种有效和可透过血脑屏障的 DREADD 激动剂,对 hM3Dq 和 hM4Di DREADDs 的 EC50 值分别为 5 nM 和 0.5 nM。JHU37152 在小鼠脑组织中表现出来自 DREADDs 的选择性 [3H]Clozapine 置换作用,而不来自其他 Clozapine 结合部位。
生物活性
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC 50 s of 5?nM and 0.5?nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
性状
Solid
IC50 & Target[1][2]
EC50: 5?nM (hM3Dq DREADD); 0.5?nM (hM4Di DREADD)
体外研究(In Vitro)
JHU37152 displays high DREADD affinity, with Kis of 1.8?nM and 8.7?nM for hM3Dq and hM4Di expressed in mouse brain sections.
JHU37152 (1-1000 nM) selectively displaces [H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
JHU37152 (0.1 mg/kg; i.p.) exhibits high DREADD occupancy in mice and rats.
JHU37152 (0.01-1 mg/kg; i.p.) selectively inhibits locomotor activity in D1-hM3Dq and D1-hM4Di mice without any significant locomotor effects observed in WT mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Bonaventura J, et, al. High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat Commun. 2019 Oct 11;10(1):4627.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (92.88 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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