1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. JHU37152

JHU37152 

Cat. No.: HY-131891
Handling Instructions

JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.

For research use only. We do not sell to patients.

JHU37152 Chemical Structure

JHU37152 Chemical Structure

CAS No. : 2369979-67-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
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10 mg USD 170 In-stock
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25 mg USD 350 In-stock
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50 mg USD 550 In-stock
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100 mg USD 950 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue[1].

IC50 & Target

EC50: 5 nM (hM3Dq DREADD); 0.5 nM (hM4Di DREADD)[1]

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[1].
JHU37152 (1-1000 nM) selectively displaces [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JHU37152 (0.1 mg/kg; i.p.) exhibits high DREADD occupancy in mice and rats[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

358.84

Formula

C₁₉H₂₀ClFN₄

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (92.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7868 mL 13.9338 mL 27.8676 mL
5 mM 0.5574 mL 2.7868 mL 5.5735 mL
10 mM 0.2787 mL 1.3934 mL 2.7868 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

JHU37152JHU 37152JHU-37152mAChRMuscarinic acetylcholine receptorDREADDhM3DqhM4DiClozapineInhibitorinhibitorinhibit

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JHU37152
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