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JHU 37160

SKU: orb1218334

Description

JHU 37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

Images & Validation

Key Properties

CAS Number2369979-68-8
MW358.85
Purity>98% (HPLC)
FormulaC19H20ClFN4
SMILESFC1=C2NC3=CC=C(Cl)C=C3N=C(N4CCN(CC)CC4)C2=CC=C1
TargetAChR
SolubilityDMSO:72 mg/mL (200.65 mM);Ethanol:72 mg/mL (200.65 mM)

Bioactivity

In Vivo
JHU37160 (0.1 mg/kg; i.p.) exhibits high DREADD occupancy in mice and rats. JHU37160 (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.
In Vitro
JHU37160 displays high DREADD affinity, with Kis of 1.9 nM and 3.6 nM for hM3Dq and hM4Di expressed in mouse brain sections. JHU37160 (1-1000 nM) selectively displaces [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information

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