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DREADD agonist 21
🥰Excellent
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
🥰Excellent
Purity: 99.88%
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 | Availability | Quantity |
|---|---|---|---|
| 2 mg | $29 | In Stock | |
| 5 mg | $53 | In Stock | |
| 10 mg | $77 | In Stock | |
| 25 mg | $143 | In Stock | |
| 50 mg | $233 | In Stock | |
| 100 mg | $347 | In Stock | |
| 200 mg | $497 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $44 | In Stock |
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- $29
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Purity:99.88%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM). |
| Targets&IC50 | M1 (human):（pki）5.97 , M4 (human):5.44（pki）, H1 receptor:（ki）6 nM, 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）, M1Dq (human):7.2（pki） |
| 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]. |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 75 mg/mL (269.44 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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