JHU 37152( —— )

Catalog No. M24084 CAS No. 2369979-67-7

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.?

Purity : >98% (HPLC)

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Biological Information

Product Name

JHU 37152
Note

Research use only, not for human use.
Brief Description

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.?
Description

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

——
Pathway

Endocrinology/Hormones
Target

AChR
Recptor

M3 mAChR
Research Area

——
Indication

——

Chemical Information

CAS Number

2369979-67-7
Formula Weight

358.85
Molecular Formula

C19H20ClFN4
Purity

>98% (HPLC)
Solubility

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

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

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1.Bonaventura J , Eldridge M , Hu F , et al. High-potency ligands for DREADD imaging and activation in rodents and monkeys[J]. Nature Communications, 2019, 10(1).

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