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SML2392 Sigma-Aldrich

DREADD Agonist 21 dihydrochloride

≥98% (HPLC)

Synonym: 11-(1-piperazinyl)-5H-Dibenzo[b,e][1,4]diazepine dihydrochloride, 11-(Piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine; 11-Piperazinyldibenzo[b,e][1,4]diazepine dihydrochloride, Compound 21 dihydrochloride

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, DIG-DY
assay   ≥98% (HPLC)
form   powder
storage condition   desiccated
color   yellow to brown
solubility   H2O: 2 mg/mL, clear
storage temp.   −20°C
SMILES string   C1(C=CC=C2)=C2C(N3CCNCC3)=NC(C=CC=C4)=C4N1

Description

Biochem/physiol Actions

Compound 21 is a potent designer drug with full agonist activity toward human hM3Dq (EC50 = 1.7 nM by cell-based Ca2+ mobilization assay), a human M3 muscarinic receptor (M3R)-based Gq (M3Dq) DREADD (Designer Receptors Exclusively Activated by Designer Drugs), displaying little activity toward muscarinic acetylcholine receptor M3 (30% M3 activation at 10 μM) and reduced affinity toward H1, 5HT2A, 5HT2C, α1A receptor (fold selectivity = 3.5, 40, 100, 165, respectively). Note: the DREADD hM3Dq exhibits M3 biological activity, but is insensitive to the endogenous ligand acetylcholine (ACh).

Safety & Documentation

Safety Information

Symbol 
GHS07  GHS07
Signal word 
Warning
Hazard statements 
Precautionary statements 
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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