DREADD Agonist 21

  Cat. No.:  DC10039   Featured
Chemical Structure
56296-18-5
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Field of application
DREADD agonist 21 is a potent muscarinic hM3Dq DREADD agonist (EC50 = 1.7 nM). Highly selective for hM3Dq DREADDs over endogenous hM3 receptors.
Cas No.: 56296-18-5
Chemical Name: DREADD agonist 21
Synonyms: 11-Piperazinyldibenzo[b,e][1,4]diazepine;DREADD Agonist 21;AK685588;11-Piperazinyldibe nzo[b,e] [1,4]diazepine;11-(piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine;11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
SMILES: N1(C2C3=C([H])C([H])=C([H])C([H])=C3N([H])C3=C([H])C([H])=C([H])C([H])=C3N=2)C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H]
Formula: C17H18N4
M.Wt: 278.3516
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
In Vitro: DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM) and does not activate human M3 receptor (hM3). 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 shows 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].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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