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DREADD agonist 21

Catalog No. T11095L CAS 56296-18-5

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

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DREADD agonist 21, CAS 56296-18-5

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1 mg	In stock	$ 33.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 239.00
50 mg	In stock	$ 389.00
100 mg	In stock	$ 579.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 98.27%

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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 , α1A-adrenoceptor:280 nM（ki）, M3Dq (human):1.7 nM (EC50), 5-HT2A receptor:66 nM（ki）, H1 receptor:（ki）6 nM, M4 (human):5.44（pki）, M1Dq (human):7.2（pki）, 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].

Molecular Weight	278.35
Formula	C17H18N4
CAS No.	56296-18-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 75 mg/mL (269.44 mM)

References and Literature

1. Chen X, et al. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84. 2. Thompson KJ, et al. DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo. ACS Pharmacol Transl Sci. 2018 Sep 14;1(1):61-72.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library NO PAINS Compound Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Serotonin Receptor-Targeted Compound Library Anti-Parkinson's Disease Compound Library

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Keywords

DREADD agonist 21 56296-18-5 GPCR/G Protein Immunology/Inflammation Neuroscience Adrenergic Receptor AChR Histamine Receptor 5-HT Receptor Muscarinic acetylcholine receptor schizophrenia mAChR Inhibitor muscarinic disease inhibit DREADD agonist21 neurodegenerative acetylcholine DREADD neuronal hM3Dq DREADD agonist-21 activation receptors inhibitor

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