2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. DREADD agonist 21

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).

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DREADD agonist 21 Chemical Structure

DREADD agonist 21 Chemical Structure

CAS No. : 56296-18-5

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Based on 1 publication(s) in Google Scholar

Other Forms of DREADD agonist 21:

DREADD agonist 21 Related Antibodies

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Description

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM)[1].

IC50 & Target

mAChR3

 

In Vitro

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM) and does not activate human M3 receptor (hM3). In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC50=1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 shows high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with Ki values of 66, 170, 280, and 6 nM, respectively[1].
DREADD agonist 21 potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 binds to hM1, hM4, hM1Dq and hM4Di receptors with pKis of 5.97, 5.44, 7.20, and 6.75, respectively. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro with a pEC50 of 8.48±0.05. DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays)[2].

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

DREADD agonist 21 Related Antibodies
In Vivo

DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice[2].
DREADD agonist 21 has excellent bioavailability, pharmacokinetic properties, and brain penetrability. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) displays 95.1% plasma protein binding and 95% brain protein bounding in mice[2].

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

278.35

Formula

C17H18N4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C12=CC=CC=C1NC3=CC=CC=C3C(N4CCNCC4)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 78 mg/mL (280.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5926 mL 17.9630 mL 35.9260 mL
5 mM 0.7185 mL 3.5926 mL 7.1852 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (8.98 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.98 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 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:

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(per animal)

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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
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5926 mL 17.9630 mL 35.9260 mL 89.8150 mL
5 mM 0.7185 mL 3.5926 mL 7.1852 mL 17.9630 mL
10 mM 0.3593 mL 1.7963 mL 3.5926 mL 8.9815 mL
15 mM 0.2395 mL 1.1975 mL 2.3951 mL 5.9877 mL
20 mM 0.1796 mL 0.8981 mL 1.7963 mL 4.4907 mL
25 mM 0.1437 mL 0.7185 mL 1.4370 mL 3.5926 mL
30 mM 0.1198 mL 0.5988 mL 1.1975 mL 2.9938 mL
40 mM 0.0898 mL 0.4491 mL 0.8981 mL 2.2454 mL
50 mM 0.0719 mL 0.3593 mL 0.7185 mL 1.7963 mL
60 mM 0.0599 mL 0.2994 mL 0.5988 mL 1.4969 mL
80 mM 0.0449 mL 0.2245 mL 0.4491 mL 1.1227 mL
100 mM 0.0359 mL 0.1796 mL 0.3593 mL 0.8981 mL
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DREADD agonist 21 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DREADD agonist 2156296-18-5DREADD agonist21DREADD agonist-21mAChRMuscarinic acetylcholine receptormuscarinicacetylcholineM3receptorshM3DqneurodegenerativediseaseschizophreniaDREADDneuronalactivationInhibitorinhibitorinhibit

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