DREADD agonist 21

SKU: orb1309741

Description

DREADD agonist 21

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	56296-18-5
MW	278.35
Purity	99.94%
Formula	C₁₇H₁₈N₄
SMILES	C1CN(CCN1)C1=Nc2ccccc2Nc2ccccc12
Target	Histamine Receptor,Adrenergic Receptor,5-HT Receptor,AChR
Solubility	DMSO:75 mg/mL (269.44 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.19 mM)

Bioactivity

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Target IC50	5 hT2C receptor:170 nM（ki）\|M4Di (human):6.75（pki）\|M1Dq (human):7.2（pki）\|M4 (human):5.44（pki）\|5 hT2A receptor:66 nM（ki）\|M1 (human):（pki）5.97 \|M3Dq (human):1.7 nM (EC50)\|α1A-adrenoceptor:280 nM（ki）\|H1 receptor:（ki）6 nM Read more...
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. Read more...
In Vitro	DREADD agonist 21 is a highly Selective and potent agonist for muscarinic DREADDs (pEC50 for hM1D = .54 and that for hM4D = .77 in pERK assays. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro (pEC50: 8.4 ± .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, respectivel. In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC5 = .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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Disclaimer	For research use only

Alternative Names

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disease, DREADD, DREADD agonist 21, DREADD agonist21, DREADD agonist-21, 5-HT2A, 5HT2A serotonin receptor 5HT2A, 5-HT2C, 5HT2C serotonin receptor, acetylcholine, Adrenergic Receptor, AdrenergicReceptor, activation, 5HTReceptor, 5HT Receptor, H1 receptor, H1 histamine receptor, Inhibitor, hM3Dq, hM4, hM4Di, hM1, hM1Dq, HistamineReceptor, Histamine Receptor, inhibit, muscarinic, Muscarinic acetylcholine receptor, M4 mAChR, M1 mAChR, mAChR, neuronal, neurodegenerative, receptors, schizophrenia, α1A-adrenergic receptor, α1A adrenergic receptor

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Compound Identifiers

PubChem CID

11818276 ↗

Key Properties

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No computed properties available.

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