JHU 37160 是一种有效的脑渗透性 DREADD 激动剂，在 HEK-293 细胞中对 hM3Dq 和 hM4Di DREADD 的 EC50 分别为 18.5 nM 和 0.2 nM。
| Cas No. | 2369979-68-8 |
| Canonical SMILES | CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=C(C=CC=C24)F)CC1 |
| 分子式 | C19H20ClFN4 |
| 分子量 | 358.85 |
| 溶解度 | DMSO|17.94|50| |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | High affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.9 nM and 3.6 nM for hM3Dq and hM4Di in vitro, respectively; EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in vitro, respectively). Displays approximately 25-fold higher affinity for hM4Di compared to DREADD agonist 21 . 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, and increases hM3Dq-stimulated locomotion in rats expressing hM3Dq in TH-expressing neurons. Brain penetrant in mice, rats and non-human primates. |
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