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

DREADD agonist 21 dihydrochloride 

Cat. No.: HY-100234A Purity: 98.53%
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DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).

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DREADD agonist 21 dihydrochloride Chemical Structure

DREADD agonist 21 dihydrochloride Chemical Structure

CAS No. : 2250025-92-2

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Based on 1 publication(s) in Google Scholar

Other Forms of DREADD agonist 21 dihydrochloride:

DREADD agonist 21 dihydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DREADD agonist 21 dihydrochloride

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Description

DREADD agonist 21 dihydrochloride 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 dihydrochloride 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

351.27

Formula

C17H20Cl2N4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Cl.[H]Cl.C1(N2CCNCC2)=NC3=C(NC4=C1C=CC=C4)C=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (569.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (284.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8468 mL 14.2341 mL 28.4681 mL
5 mM 0.5694 mL 2.8468 mL 5.6936 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.8468 mL 14.2341 mL 28.4681 mL 71.1703 mL
5 mM 0.5694 mL 2.8468 mL 5.6936 mL 14.2341 mL
10 mM 0.2847 mL 1.4234 mL 2.8468 mL 7.1170 mL
15 mM 0.1898 mL 0.9489 mL 1.8979 mL 4.7447 mL
20 mM 0.1423 mL 0.7117 mL 1.4234 mL 3.5585 mL
25 mM 0.1139 mL 0.5694 mL 1.1387 mL 2.8468 mL
30 mM 0.0949 mL 0.4745 mL 0.9489 mL 2.3723 mL
40 mM 0.0712 mL 0.3559 mL 0.7117 mL 1.7793 mL
50 mM 0.0569 mL 0.2847 mL 0.5694 mL 1.4234 mL
60 mM 0.0474 mL 0.2372 mL 0.4745 mL 1.1862 mL
80 mM 0.0356 mL 0.1779 mL 0.3559 mL 0.8896 mL
100 mM 0.0285 mL 0.1423 mL 0.2847 mL 0.7117 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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DREADD agonist 21 dihydrochloride 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 212250025-92-2DREADD agonist21DREADD agonist-21mAChRMuscarinic acetylcholine receptormuscarinicacetylcholineM3receptorshM3DqneurodegenerativediseaseschizophreniaDREADDneuronalactivationInhibitorinhibitorinhibit

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