Deschloroclozapine

Name: Deschloroclozapine
Brand: MedChemExpress
SKU: HY-42110
Rating: 5.0 (42 reviews)

Cat. No.: HY-42110 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with K_i 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

CAS No. : 1977-07-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 64	In-stock	Estimated Time of Arrival: December 31
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
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 42 publication(s) in Google Scholar

Other Forms of Deschloroclozapine:

Deschloroclozapine dihydrochloride Get quote

42 Publications Citing Use of MCE Deschloroclozapine

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All mAChR Isoform Specific Products:

View All Isoforms

mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

mAChR3

mAChR4

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].

MedChemExpress (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].

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

Molecular Weight

292.38

Formula

C₁₈H₂₀N₄

CAS No.

1977-07-7

Appearance

Solid

Color

Light yellow to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

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
Protocol 4

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
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (257 KB) HNMR (251 KB) RP-HPLC (242 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Maggs JL, et al. The metabolic formation of reactive intermediates from clozapine, a drug associated with agranulocytosis in man. J Pharmacol Exp Ther. 1995;275(3):1463-1475. [Content Brief]

[2]. Hu F, et al. ¹⁸F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography. Eur J Med Chem. 2021;213:113047. [Content Brief]

[3]. Upright NA, et al. Effect of chemogenetic actuator drugs on prefrontal cortex-dependent working memory in nonhuman primates. Neuropsychopharmacology. 2020;45(11):1793-1798. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4202 mL	17.1010 mL	34.2021 mL	85.5052 mL
	5 mM	0.6840 mL	3.4202 mL	6.8404 mL	17.1010 mL
	10 mM	0.3420 mL	1.7101 mL	3.4202 mL	8.5505 mL
	15 mM	0.2280 mL	1.1401 mL	2.2801 mL	5.7003 mL
	20 mM	0.1710 mL	0.8551 mL	1.7101 mL	4.2753 mL
	25 mM	0.1368 mL	0.6840 mL	1.3681 mL	3.4202 mL
	30 mM	0.1140 mL	0.5700 mL	1.1401 mL	2.8502 mL
	40 mM	0.0855 mL	0.4275 mL	0.8551 mL	2.1376 mL
	50 mM	0.0684 mL	0.3420 mL	0.6840 mL	1.7101 mL
	60 mM	0.0570 mL	0.2850 mL	0.5700 mL	1.4251 mL
	80 mM	0.0428 mL	0.2138 mL	0.4275 mL	1.0688 mL
	100 mM	0.0342 mL	0.1710 mL	0.3420 mL	0.8551 mL