1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Deschloroclozapine

Deschloroclozapine 

Cat. No.: HY-42110 Purity: 99.59%
Handling Instructions

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.

For research use only. We do not sell to patients.

Deschloroclozapine Chemical Structure

Deschloroclozapine Chemical Structure

CAS No. : 1977-07-7

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Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

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Description

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging[1][2][3].

IC50 & Target

Ki: 6.3 nM (hM3Dq), 4.2 nM (hM4Di)[2]

In Vitro

Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a chemogenetic approach for remote manipulation of neuronal activity in freely-moving animals. DREADDs comprise mutated G protein-coupled receptors (GPCRs) that do not respond to their endogenous neurotransmitter, but do respond to an otherwise “inert” exogenous substance[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Deschloroclozapine (0.3 mg/kg; intramuscularly) impairs working memory function in male rhesus macaques (aged between 5 and 6 years and weighing 5.5-7.9 kg)[3].
Deschloroclozapine (0.1 mg/kg; i.m) is effective at activating DREADD receptors in vivo and reversibly inducing behavioral effects in monkeys[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

292.38

Formula

C18H20N4

CAS No.
SMILES

CN1CCN(C2=NC3=CC=CC=C3NC4=CC=CC=C42)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (342.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4202 mL 17.1010 mL 34.2021 mL
5 mM 0.6840 mL 3.4202 mL 6.8404 mL
10 mM 0.3420 mL 1.7101 mL 3.4202 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 5.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
Deschloroclozapine
Cat. No.:
HY-42110
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