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DREADD agonist 21

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Purity:98.27%

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COA HNMR HPLC

DREADD agonist 21

Catalog No. T11095LCas No. 56296-18-5

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

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Pack Size	Price	Availability
1 mg	$33	In Stock
2 mg	$47	In Stock
5 mg	$89	In Stock
10 mg	$128	In Stock
25 mg	$239	In Stock
50 mg	$389	In Stock
100 mg	$579	In Stock
1 mL x 10 mM (in DMSO)	$74	In Stock

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Product Introduction

Bioactivity

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

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 75 mg/mL (269.44 mM)

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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