| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
EC50: 5 nM (hM3Dq DREADD); 0.5 nM (hM4Di DREADD)[1]
hM3Dq and hM4Di DREADD (Designer Receptors Exclusively Activated by Designer Drugs) receptors. JHU37152 is a potent and selective agonist at these engineered G protein-coupled receptors. |
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| ln Vitro |
With Kis of 1.8 nM and 8.7 nM for hM3Dq and hM4Di expressed in mouse brain slices, respectively, JHU37152 exhibits strong DREADD affinity[1]. [3H]Clozapine displacement from DREADDs is selectively displaced by JHU37152 (1-1000 nM), but not from other Clozapine-binding sites[1].
JHU37152 is a potent DREADD agonist with EC50 values of 5 nM for hM3Dq and 0.5 nM for hM4Di in HEK-293 cell-based assays. It exhibits high binding affinity with Ki values of 1.8 nM for hM3Dq and 8.7 nM for hM4Di. The compound displaces [3H]clozapine from DREADDs, confirming its specific interaction with these engineered receptors. No responses are observed in untransfected HEK-293 cells, demonstrating its selectivity for DREADD receptors over endogenous targets. |
| ln Vivo |
In mice and rats, JHU37152 (0.1 mg/kg; ip) shows strong DREADD occupancy[1]. Without significantly affecting WT mice's locomotor activity, JHU37152 (0.01–1 mg/kg; ip) specifically suppresses locomotor activity in D1–hM3Dq and D1–hM4Di mice[1].
In vivo, JHU37152 exhibits high DREADD occupancy in mice and rats at a dose of 0.1 mg/kg (i.p.). At doses ranging from 0.01 to 1 mg/kg (i.p.), the compound selectively inhibits locomotor activity in D1-hM3Dq and D1-hM4Di mice. The compound exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from wild-type and D1-DREADD mice. JHU37152 has been used in combination with PET imaging using [18F]JHU37107 to allow for DREADD detection in locally-targeted neurons. |
| Enzyme Assay |
In vitro receptor binding assays are performed to determine the affinity of JHU37152 for hM3Dq and hM4Di DREADD receptors. Radioligand binding studies using membrane preparations from cells expressing the DREADD receptors are conducted. The compound's ability to displace [3H]clozapine from the receptors is measured to calculate its Ki values. The selectivity of JHU37152 for DREADD receptors over endogenous targets is confirmed by testing its activity in untransfected cells.
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| Cell Assay |
In vitro cell-based assays are conducted using HEK-293 cells expressing hM3Dq or hM4Di DREADD receptors. The cells are treated with varying concentrations of JHU37152, and receptor activation is measured by assessing downstream signaling events such as calcium mobilization in fluorescent assays or BRET-based assays. The EC50 values are determined from the concentration-response curves. No responses are observed in untransfected HEK-293 cells, confirming the selectivity of the compound.
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| Animal Protocol |
In vivo studies are conducted in rodent models to evaluate the pharmacological effects of DREADD activation using JHU37152. The compound is typically administered via intraperitoneal injection at doses ranging from 0.01 to 1 mg/kg. Its effects on locomotor activity are assessed in D1-hM3Dq and D1-hM4Di mice. DREADD occupancy is measured in brain tissue to confirm target engagement. The compound has also been used in combination with PET imaging for DREADD detection in vivo.
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| ADME/Pharmacokinetics |
JHU37152 is a brain-penetrant compound that exhibits high in vivo DREADD potency. The compound's ability to cross the blood-brain barrier and its high DREADD occupancy in the brain have been demonstrated in mice and rats. Brain and serum concentrations and ratios of JHU37152 have been characterized in mice at different time points after a 0.1 mg/kg intraperitoneal injection. These data support its use as a potent and efficacious DREADD agonist for in vivo neuroscience research.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for JHU37152. As a DREADD agonist, its toxicity profile is expected to be related to its mechanism of action, which depends on the specific DREADD receptor being activated. The compound shows no activity in untransfected cells, suggesting low off-target toxicity. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
JHU37152 is a potent, brain-penetrant DREADD agonist that is widely used in neuroscience research for chemogenetic modulation of neuronal activity. Its high potency (EC50 = 5 nM for hM3Dq and 0.5 nM for hM4Di) and selectivity make it a valuable tool for studying the function of specific neuronal populations in vivo. The compound is not approved for human therapeutic use and is strictly for research purposes. JHU37152 is also known as JHU 37152 and is available as a high-purity research reagent.
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| Molecular Formula |
C19H20CLFN4
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|---|---|
| Molecular Weight |
358.8403
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| Exact Mass |
358.136
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| CAS # |
2369979-67-7
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| PubChem CID |
139033721
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| Appearance |
White to yellow solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
494
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C2=C(C=1[H])N=C(C1C(=C([H])C([H])=C([H])C=1N2[H])F)N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C1([H])[H]
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| InChi Key |
NZMZJNNWMSYDNX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20ClFN4/c1-2-24-8-10-25(11-9-24)19-18-14(21)4-3-5-16(18)22-15-7-6-13(20)12-17(15)23-19/h3-7,12,22H,2,8-11H2,1H3
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| Chemical Name |
3-chloro-6-(4-ethylpiperazin-1-yl)-7-fluoro-11H-benzo[b][1,4]benzodiazepine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 33.33 mg/mL (92.88 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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