JHU 37152

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JHU 37152 是一种仅由设计药物 (DREADD) 激动剂激活的设计受体，体外人毒蕈碱乙酰胆碱 M3 受体 (hM3Dq) 和 hM4Di 的 Ki 值分别为 1.8 nM 和 8.7 nM。

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.

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 [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites.

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.

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Endocrinology/Hormones

AChR

M3 mAChR

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2369979-67-7

358.85

C19H20ClFN4

>98% (HPLC)

DMSO:72 mg/mL (200.65 mM);Ethanol:24 mg/mL (66.88 mM)

FC1=C2C(NC3=CC=C(Cl)C=C3N=C2N4CCN(CC)CC4)=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years