1. GPCR/G Protein Neuronal Signaling
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  3. JHU37152

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.

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JHU37152 Chemical Structure

JHU37152 Chemical Structure

CAS No. : 2369979-67-7

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10 mM * 1 mL in DMSO
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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].

MedChemExpress (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].

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

Molecular Weight

358.84

Formula

C19H20ClFN4

CAS No.
Appearance

Solid

Color

White to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7868 mL 13.9338 mL 27.8676 mL 69.6689 mL
5 mM 0.5574 mL 2.7868 mL 5.5735 mL 13.9338 mL
10 mM 0.2787 mL 1.3934 mL 2.7868 mL 6.9669 mL
15 mM 0.1858 mL 0.9289 mL 1.8578 mL 4.6446 mL
20 mM 0.1393 mL 0.6967 mL 1.3934 mL 3.4834 mL
25 mM 0.1115 mL 0.5574 mL 1.1147 mL 2.7868 mL
30 mM 0.0929 mL 0.4645 mL 0.9289 mL 2.3223 mL
40 mM 0.0697 mL 0.3483 mL 0.6967 mL 1.7417 mL
50 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3934 mL
60 mM 0.0464 mL 0.2322 mL 0.4645 mL 1.1611 mL
80 mM 0.0348 mL 0.1742 mL 0.3483 mL 0.8709 mL
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JHU37152 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JHU37152
Cat. No.:
HY-131891
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