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JHU37152 dihydrochloride (DREADD ligand) (water soluble)

(HB6253)
Data

Product overview

  • Name
    JHU37152 dihydrochloride (DREADD ligand) (water soluble)
  • Short description

    Novel DREADD agonist with high affinity and potency for hM3Dq and hM4Di. Active in vivo. Water soluble.

  • Biological description

    Overview

    JHU37152 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 1.8 nM (hM3Dq) and 8.7 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.

    JHU37152 activates hM3Dq and hM4Di with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells (EC50 values are 5 and 0.5 nM at hM3Dq and hM4Di respectively.

    Occupancy

    JHU37152 exhibits high in vivo DREADD occupancy and was not reported to be a P-gp substrate.

    In vivo application

    JHU37152 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).

    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.

    Freebase also available.

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

  • Alternative names
    J52 dihydrochloride
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    8-chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
  • Molecular Weight
    431.76
  • Chemical structure
    JHU37152 dihydrochloride
  • Molecular Formula
    C19H20ClFN4 · 2HCl
  • PubChem identifier
    0
  • SMILES
    Cl.Cl.CCN1CCN(CC1)C2=Nc4cc(Cl)ccc4Nc3cccc(F)c23
  • Source
    Synthetic
  • InChi
    InChI=1S/C19H20ClFN4.2ClH/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;2*1H
  • InChiKey
    FCMLDQBEZPOLPW-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 JHU37152 dihydrochloride (DREADD ligand) (water soluble)

  • Chemogenetic ligands for translational neurotheranostics

    Bonaventura et al (2018) bioRxiv : doi: https://doi.org/10.1101/487
  • High-potency ligands for DREADD imaging and activation in rodents and monkeys.

    Bonaventura et al (2019) Nat Commun. 10(1) : 4627
    PubMedID: 31604917
  • 0067 Humanized Chemogenetic Approach to Treat Sleep Apnea

    Curado et al (2019) Sleep (42) : A28
  • OP-01-02 Graft-host synaptic connectivity can be chemogenetically inhibited with clinically relevant activators to eliminate graft-induced dyskinesias (GID) without loosing anti-parkinsonian benefits of dopaminergic grafts

    Subramanian et al (2019) World Congress On Parkinson's Disease And Related Disorders 2019 : Poster Abstract
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