JHU37152 是一种可透过血脑屏障的DREADD激动剂。 在 HEK-293 细胞的荧光和基于 BRET 的测定中,对hM3Dq和hM4Di DREADDs的EC50值分别为 5 和 0.5 nM。
产品描述
JHU 37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
体外活性
JHU 37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells
体内活性
JHU 37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice
Cas No.
2369979-67-7
分子式
C19H20ClFN4
分子量
358.85
别名
JHU 37152;JHU37152
储存和溶解度
Ethanol:24 mg/mL (66.88 mM)
DMSO:72 mg/mL (200.65 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years