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JHU37160 dihydrochloride (DREADD ligand) (water soluble)

(HB6261)
Data

Product overview

  • Name
    JHU37160 dihydrochloride (DREADD ligand) (water soluble)
  • Short description
    Novel DREADD ligand with high affinity and potency for hM3Dq and hM4Di. Active in vivo. Water soluble.
  • Biological description

    JHU37160 is a novel DREADD ligand with high affinity and potency for hM3Dq and hM4Di (Ki values are 1.9 nM (hM3Dq) and 3.6 nM (hM4Di).


    It displays high potency and efficacy in fluorescent and BRET-based assays (EC50 values are 18.5 nM (hM3Dq) and 0.2 nM (hM4Di).


    JHU37160 is reported to be a potent in vivo DREADD agonist, selectively inhibiting locomotor activity in D1-hM3Dq and D1-hM4Di mice at doses of 0.01 - 1 mg/kg (i.p), with no significant activity in non-DREADD expressing (wildtype) mice.


    JHU37160 also displays high in vivo DREADD occupancy (as measured by displacement of [11]Clozapine DREADD binding in vivo in various species).


    Freebase also available.


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

  • Alternative names
    J60 dihydrochloride
  • Purity
    >98%
  • Citations

Properties

  • 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
  • Molecular Formula
    C19H20ClFN4 · 2HCl
  • 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

Storing and Using Your Product

  • 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.
  • Handling continued..


    Storage of solutions at room temperature

    • We recommend only keeping solutions at room temperature (25°C) for a few days as our studies have shown that after 96 hours the purity of the compound in solution drops to ~95% and will continue to drop over time.
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

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

  • Chemogenetic ligands for translational neurotheranostics

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