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JHU37160 dihydrochloride (DREADD ligand) (water soluble)

(HB6261)
Technical documents: SDS CoA Datasheet

Product overview

Name JHU37160 dihydrochloride (DREADD ligand) (water soluble)
Alternative names J60 dihydrochloride
Purity >98%
Description Novel DREADD agonist with high affinity and potency for hM3Dq and hM4Di. Active in vivo. Water soluble.
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JHU37160 dihydrochloride (DREADD ligand) (water soluble) product vial image | Hello Bio

Biological Data

Biological description

Overview

JHU37160 is reported to be a novel DREADD agonist with high in vivo DREADD potency for CNS applications.

It has high affinity in vitro for hM3Dq and hM4Di (Ki values are 1.9 nM (hM3Dq) and 3.6 nM (hM4Di).

It selectively displaces [3H]clozapine from DREADDs and not from other clozapine-binding sites at concentrations up to 10 nM when tested for in situ [3H]clozapine displacement in brain tissue from WT and D1-DREADD mice.

JHU37160 activates hM3Dq and hM4Di with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells (EC50 values are 18.5 and 0.2 nM at hM3Dq and hM4Di respectively.

Occupancy

JHU37160 exhibits high in vivo DREADD occupancy and was not reported to be a P-gp substrate.

In vivo application

JHU37160 is reported to be a potent in vivo DREADD agonist, which selectively inhibits locomotor activity in D1-hM3Dq and D1-hM4Di mice without any significant locomotor effects observed in wild type (WT) mice (at doses ranging 0.01 - 1 mg/kg).

It also produces robust and selective increases in hM3Dq-stimulated locomotion in rats expressing hM3Dq in tyrosine hydroxylase expressing neurons (at doses ranging 0.01 – 0.3 mg/kg).

In in vivo electrophysiology experiments in mice, JHU37160 produces rapid and potent hM4Di-driven inhibition of light-evoked neuronal activation (at a dose of 0.1 mg/kg).

While its selectivity is not ideal (i.e. comparable to clozapine), its high in vivo potency allows for dose adjustments with minimal off-target effects. The compound exhibits promising characteristics for DREADD use in monkeys.

Shows dose-dependent anxiogenic effect in male Wistar and Long-Evans rats, regardless of DREADD expression, with no impact on locomotor behvaiour suggesting that high doses (e.g. 1mg/kg) should be avoided in chemogenetic experiments designed to evaluate circuit manipulation on anxiety-like behavior in rats.

Freebase also available.

Sold under license from the NIH, US patent pending 62/627,527


Stability Studies

For more info on the stability of water-soluble DREADD ligands in solution, please see the following guides:

Solubility & Handling

Storage instructions -20°C
Solubility overview Soluble in water (100mM). Always store solutions at -20°C.
Handling

Storage of solid

  • Store at -20°C.
  • Please note that the compound is a hydroscopic solid and contact with air may cause material to become sticky. Product performance should not be affected but we recommend storing the material in a sealed jar.

Storage of solutions

  • Make up solutions and use immediately.
  • If storage of solutions is required, you should aliquot out the solution into tightly sealed vials and store at -20°C and store these for up to one month.
  • Allow the product to equilibrate to RT for at least one hour before opening and using.


Storage of solutions at room temperature

  • We have found that this compound precipitates in aqueous solution at RT (˜25°C)
  • We therefore recommend that you make up solutions and use immediately.
  • Always check that your product is completely dissolved before use.
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

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Dilution

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Chemical Data

Purity >98%
Chemical name 8-chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
Molecular Weight 431.76
Chemical structure JHU37160 dihydrochloride Chemical Structure
Molecular Formula C19H20ClFN4 · 2HCl
CAS Number 2369979-68-8 (free base)
SMILES Cl.Cl.CCN1CCN(CC1)C3=Nc4cc(Cl)ccc4Nc2c3cccc2F
Source Synthetic
InChi InChI=1S/C19H20ClFN4.2ClH/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;2*1H
InChiKey DHICOGMHOCAKOF-UHFFFAOYSA-N
Appearance Yellow solid
Licensing details Sold under license from the NIH, US patent pending 62/627,527

References for JHU37160 dihydrochloride (DREADD ligand) (water soluble)

References are publications that support the biological activity of the product
  • Chemogenetic ligands for translational neurotheranostics

    Bonaventura et al (2018) bioRxiv : doi: https://doi.org/10.1101/487

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Publications
These publications cite the use of JHU37160 dihydrochloride (DREADD ligand) (water soluble) purchased from Hello Bio:
  • Tissue-specific modification of cellular bioelectrical activities using the chemogenetic tool, DREADD, in zebrafish

    Zhang et al (2021) bioRxiv https://doi.org/10.1101/2021.06.22.449481 : doi
  • The orbitofrontal cortex is necessary for learning to ignore

    Costa KM et al (2021) Curr Biol 31(12) : 2652-2657.e3
    PubMedID: 33848459
  • Extinction blunts paraventricular thalamic contributions to heroin relapse

    Giannotti G et al (2021) Cell Rep 36(8) : 109605
    PubMedID: 34433067
  • Activation of septal OXTr neurons induces anxiety- but not depressive-like behaviors

    Huang T et al (2021) Mol Psychiatry 26(12) : 7270-7279
    PubMedID: 34489531
  • Cocaine shifts dopamine D2 receptor sensitivity to gate conditioned behaviors

    Gong S et al (2021) Neuron 109(21) : 3421-3435.e5
    PubMedID: 34506723

Items 6 to 10 of 18 total

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