| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
JHU-37160 targets DREADDs, which are engineered G protein-coupled receptors that are selectively activated by otherwise inert synthetic ligands. Specifically, it targets hM3Dq (a Gq-coupled DREADD) and hM4Di (a Gi-coupled DREADD). DREADDs are used in chemogenetics to remotely control neuronal activity and signaling pathways in vivo. JHU-37160 binds to these receptors with high affinity and potency, activating downstream signaling cascades. Its brain-penetrant properties make it suitable for in vivo chemogenetic studies.
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| ln Vitro |
JHU37160 exhibits strong affinity for DREADD; for hM3Dq and hM4Di expressed in mouse brain slices, its Kis values are 1.9 nM and 3.6 nM, respectively [1]. JHU37160 (1-1000 nM) selectively displaces additional clozapine binding sites [1] but not the [3H]clozapine displacer in DREADD.
In vitro, JHU-37160 activates hM3Dq and hM4Di DREADDs in HEK-293 cells with EC50 values of 18.5 nM and 0.2 nM, respectively. It displays approximately 25-fold higher affinity for hM4Di compared to DREADD agonist 21. The compound's high potency and selectivity for DREADDs make it a valuable tool for chemogenetic studies in neuroscience and cell biology. It can be used to activate DREADD-expressing cells in vitro and in vivo. |
| ln Vivo |
JHU37160 (0.1 mg/kg; i.p.) displays strong DREADD occupancy in mice and rats [1]. JHU37160 (0.01-1 mg/kg; i.p.) specifically reduces locomotor activity in D1-hM3Dq and D1-hM4Di mice, although no evident locomotor effects were seen in WT mice [1].
In vivo, JHU-37160 is a potent and brain-penetrant DREADD agonist. It has been used in rats and non-human primates for chemogenetic studies. The compound's ability to cross the blood-brain barrier and activate DREADDs in the central nervous system makes it suitable for studying neuronal circuits and behavior. Its high potency (EC50 = 0.2 nM for hM4Di) allows for low-dose administration, minimizing off-target effects. |
| Enzyme Assay |
For in vitro receptor activation assays, HEK-293 cells expressing hM3Dq or hM4Di DREADDs are seeded in 96-well plates. Cells are treated with JHU-37160 at various concentrations (0.001-1000 nM) for 30-60 minutes. Receptor activation is measured by quantifying downstream signaling: for hM3Dq (Gq-coupled), intracellular calcium mobilization is measured using calcium-sensitive fluorescent dyes (such as Fluo-4); for hM4Di (Gi-coupled), inhibition of forskolin-stimulated cAMP accumulation is measured using cAMP ELISA or HTRF assays. EC50 values are calculated from dose-response curves.
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| Cell Assay |
For cell-based assays, cells expressing DREADDs are treated with JHU-37160 at concentrations ranging from 0.01-1000 nM. Downstream signaling pathways (calcium mobilization, cAMP levels, ERK phosphorylation) are measured. Cell morphology, gene expression, or other functional readouts can be assessed depending on the experimental design. The compound is typically used at nanomolar to low micromolar concentrations for in vitro studies.
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| Animal Protocol |
For in vivo studies, JHU-37160 is administered to rodents or non-human primates via intraperitoneal or subcutaneous injection at doses typically ranging from 0.01-1 mg/kg. The compound's brain penetration allows for activation of DREADDs expressed in specific brain regions. Behavioral assays, electrophysiological recordings, or imaging studies can be performed to assess the effects of DREADD activation. The compound's high potency allows for low-dose administration, reducing the risk of off-target effects.
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| ADME/Pharmacokinetics |
JHU-37160 is a brain-penetrant DREADD agonist with favorable pharmacokinetic properties. The compound is soluble in DMSO and other organic solvents. Storage is recommended at -20°C for long-term stability. For in vivo administration, it can be formulated in saline or other appropriate vehicles. The compound's high potency and brain penetration make it suitable for in vivo chemogenetic studies.
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| Toxicity/Toxicokinetics |
Toxicological data for JHU-37160 have not been extensively reported, as it is a research tool for chemogenetics rather than a therapeutic agent. At the low doses used for DREADD activation (0.01-1 mg/kg), the compound is generally well-tolerated in animal studies. Standard safety precautions should be followed when handling this compound. It is not intended for human use.
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| References | |
| Additional Infomation |
JHU-37160 is a potent and brain-penetrant DREADD agonist with EC50 values of 18.5 nM (hM3Dq) and 0.2 nM (hM4Di). It displays high affinity for hM4Di and is used for chemogenetic studies in neuroscience. JHU-37160 has been used in rats and non-human primates. It is a research tool and is not approved for clinical use.
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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 # |
2369979-68-8
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| PubChem CID |
139033723
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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([H])=C([H])C([H])=C(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 |
SWSCWOSASZXIRK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20ClFN4/c1-2-24-8-10-25(11-9-24)19-14-4-3-5-15(21)18(14)22-16-7-6-13(20)12-17(16)23-19/h3-7,12,22H,2,8-11H2,1H3
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| Chemical Name |
3-chloro-6-(4-ethylpiperazin-1-yl)-10-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 : ~50 mg/mL (~139.34 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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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