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Compound 21 (DREADD agonist 21) dihydrochloride (water soluble)

(HB6124)
Data

Product overview

  • Name
    Compound 21 (DREADD agonist 21) dihydrochloride (water soluble)
  • Short description
    Compound 21 has been indicated to be a highly potent hM3Dq DREADD agonist. Water soluble.
  • Biological description

    Compound 21 (DREADD agonist 21) hydrochloride is a water soluble analog of clozapine N-oxide (CNO). The Free base is also available.


    Compound 21 (DREADD agonist 21) has been indicated to be a highly potent agonist at the excitatory hM3Dq DREADD (EC50 = 1.7 nM) and shows high selectivity for activating hM3Dq compared to the native hM3 muscarinic receptor and other GPCRs.


    There are indications that Compound 21 cannot be metabolized via normal routes to clozapine (or any related compound), has minimal off-target activity and has equivalent potency in vivo when compared with clozapine N-oxide (CNO).


    Unpublished data indicates that Compound 21 (DREADD agonist 21) activates the inhibitory hM4D DREADD.

    Unpublished data also suggests using a dose of 3mg/kg in rat models.


    Data from a poster presented at SfN by the Michaelides group indicates that Compound 21 has lower binding affinity for DREADDs compared to clozapine and that Compound 21 induces behavioural effects in transgenic mice. 1mg/kg doses were used. High doses (10mg/kg) may cause sedation.

    Compound 21 may therefore represent an alternative to CNO.

  • Alternative names
    C21
  • Purity
    >98%
  • Customer comments

    We used Compound 21 (DREADD agonist 21) dihydrochloride (water soluble) (1mg/kg) and CNO in rats (1mg/kg) and we found a great effect on cells infected with dreadds-Gs. Both products are really easy to dissolve in saline! Verified customer, Universite de Bordeaux

  • Citations

Images

Properties

  • Chemical name
    11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
  • Molecular Weight
    352.29
  • Chemical structure
    Compound 21 hydrochloride
  • Molecular Formula
    C17H18N4.2HCl
  • SMILES
    C1CN(CCN1)C2=NC3=CC=CC=C3NC4=CC=CC=C42.Cl.Cl
  • Source
    Synthetic
  • InChi
    InChI=1S/C17H18N4.2ClH/c1-2-6-14-13(5-1)17(21-11-9-18-10-12-21)20-16-8-4-3-7-15(16)19-14;;/h1-8,18-19H,9-12H2;2*1H
  • InChiKey
    SETCOPAXYQJWKI-UHFFFAOYSA-N
  • Appearance
    Yellow solid

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.

    • 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 ~97% 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 Compound 21 (DREADD agonist 21) dihydrochloride (water soluble)

  • The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs.

    Chen et al (2015) ACS Chem Neurosci 6(3) : 476-84
    PubMedID: 25587888
  • Optogenetic approaches for dissecting neuromodulation and GPCR signaling in neural circuits.

    Spangler and Bruchas (2017) Curr Opin Pharmacol 32(4) : 56-70.
    PubMedID: 27875804
  • Clozapine N-Oxide Administration Produces Behavioral Effects in Long-Evans Rats: Implications for Designing DREADD Experiments.

    MacLaren et al (2016) eNeuro 3(5) : 0219-16
    PubMedID: 27822508
  • New non-CNO actuators for DREADDs

    Roth Bl (2015) Blog : N/A
Support & Resources

Reviews

  • Verified customer, Florida Atlantic University

    Great Product!, Product was delivered promptly. Very easy to work with. No problems keeping it in solution.
  • Verified customer, UT Southwestern

    Our lab tested Compound 21 (DREADD agonist 21) dihydrochloride and perlapine at 1 mg/kg (i.p.) in mice and compared its effects to that of CNO and clozapine. Compound 21, perlapine, CNO and clozapine (from Hello Bio) all effectively produced the anticipated phenotype in our DREADD-Gq animals, but not in control non-DREADD animals. The effects produced with clozapine and CNO were greater than with compound 21 and perlapine, likely due to higher affinity to DREADDs. We also noticed that the effects of compound 21 and CNO were more prolonged than that of perlapine and clozapine, perhaps due to delayed retroconversion. Overall, all of the aforementioned compounds appear suitable for chemogenetics studies, providing well-controlled experiments are used.
  • Veriried researcher, Universite de Bordeaux

    We used Compound 21 (DREADD agonist 21) dihydrochloride (water soluble) (1mg/kg) and CNO in rats (1mg/kg) and we found a great effect on cells infected with dreadds-Gs. Both products are really easy to dissolve in saline!