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JHU37152 (DREADD ligand)

(HB6252)
Data

Product overview

  • Name
    JHU37152 (DREADD ligand)
  • Short description
    Novel DREADD ligand with high affinity and potency for hM3Dq and hM4Di. Active in vivo. Freebase.
  • Biological description

    JHU37152 is a novel DREADD ligand with high affinity and potency for hM3Dq and hM4Di (Ki values are 1.8 nM (hM3Dq) and 8.7 nM (hM4Di).


    It displays high potency and efficacy in fluorescent and BRET-based assays (EC50 values are 5 nM (hM3Dq) and 0.5 nM (hM4Di).


    JHU37152 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.


    JHU37152 also displays high in vivo DREADD occupancy (as measured by displacement of [11]Clozapine DREADD binding in vivo in various species).


    Water soluble version also available.


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

  • Alternative names
    J52
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    8-chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine
  • Molecular Weight
    358.84
  • Chemical structure
    JHU37152 | Hello Bio
  • Molecular Formula
    C19H20ClFN4
  • SMILES
    CCN1CCN(CC1)C2=Nc4cc(Cl)ccc4Nc3cccc(F)c23
  • Source
    Synthetic
  • InChi
    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
  • InChiKey
    NZMZJNNWMSYDNX-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
    Room temperature
  • Solubility overview
    Soluble in DMSO (100 mM)
  • 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 JHU37152 (DREADD ligand)

  • Chemogenetic ligands for translational neurotheranostics

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