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SML2392

Sigma-Aldrich

DREADD Agonist 21 dihydrochloride

≥98% (HPLC), powder, DREADD agonist

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C17H18N4 · 2HCl
CAS Number:
Molecular Weight:
351.27
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

product name

DREADD Agonist 21 dihydrochloride, ≥98% (HPLC)

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

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).

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Precautionary Statements

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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The Journal of neuroscience : the official journal of the Society for Neuroscience, 43(28), 5221-5240 (2023-06-21)
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Moawiah M Naffaa et al.
Cell reports, 42(7), 112783-112783 (2023-07-09)
Neurogenesis and differentiation of neural stem cells (NSCs) are controlled by cell-intrinsic molecular pathways that interact with extrinsic signaling cues. In this study, we identify a circuit that regulates neurogenesis and cell proliferation in the lateral ventricle-subventricular zone (LV-SVZ). Our
Yoshiko Nakamura et al.
Science advances, 8(51), eadd5463-eadd5463 (2022-12-24)
The bidirectional controller of the thermoregulatory center in the preoptic area (POA) is unknown. Using rats, here, we identify prostaglandin EP3 receptor-expressing POA neurons (POAEP3R neurons) as a pivotal bidirectional controller in the central thermoregulatory mechanism. POAEP3R neurons are activated

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