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DREADD agonist 21

Name: DREADD agonist 21
Brand: TargetMol
SKU: T11095L
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11095LCas No. 56296-18-5

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

DREADD agonist 21

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Purity: 99.94%

Catalog No. T11095LCas No. 56296-18-5

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

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$37	In Stock	In Stock
10 mg	$54	In Stock	In Stock
25 mg	$100	In Stock	In Stock
50 mg	$163	In Stock	In Stock
100 mg	$243	In Stock	In Stock
200 mg	$348	-	In Stock
1 mL x 10 mM (in DMSO)	$31	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.94%

Appearance:Solid

Color:White

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COA LCMS HPLC HNMR

Product Introduction

Bioactivity

Description	DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).
Targets&IC50	M1Dq (human):7.2（pki）, M1 (human):（pki）5.97 , H1 receptor:（ki）6 nM, M4 (human):5.44（pki）, M3Dq (human):1.7 nM (EC50), 5-HT2A receptor:66 nM（ki）, α1A-adrenoceptor:280 nM（ki）, M4Di (human):6.75（pki）, 5-HT2C receptor:170 nM（ki）
In vitro	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]. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro (pEC50: 8.48±0.05) and it also potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 does not activate human M3 receptor (hM3). DREADD agonist 21 displays 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]. 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 binds to hM1, hM4, hM1Dq and hM4Di receptors (pKis of 5.97, 5.44, 7.20, and 6.75, respectively).
In vivo	DREADD agonist 21 has excellent pharmacokinetic properties, bioavailability and brain penetrability. DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) shows 95.1% plasma protein binding and 95% brain protein bounding in mice[2].

Chemical Properties

Molecular Weight	278.35
Formula	C₁₇H₁₈N₄
Cas No.	56296-18-5
Smiles	C1CN(CCN1)C1=Nc2ccccc2Nc2ccccc12
Relative Density.	1.28 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 75 mg/mL (269.44 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.19 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5926 mL	17.9630 mL	35.9260 mL	179.6300 mL
5 mM	0.7185 mL	3.5926 mL	7.1852 mL	35.9260 mL
10 mM	0.3593 mL	1.7963 mL	3.5926 mL	17.9630 mL
20 mM	0.1796 mL	0.8981 mL	1.7963 mL	8.9815 mL
50 mM	0.0719 mL	0.3593 mL	0.7185 mL	3.5926 mL
100 mM	0.0359 mL	0.1796 mL	0.3593 mL	1.7963 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc