SML2022
UCSF924
≥98% (HPLC)
Synonym(s):
6-Methyl-2-((3-phenoxypropylamino)methyl)quinolin-4(1H)-one, ZINC000091726127
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5 MG
$128.25
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$545.00
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List Price$135.00Save 5%Web-Only Promotion
Available to ship onApril 28, 2025Details
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5 MG
$128.25
25 MG
$545.00
About This Item
Empirical Formula (Hill Notation):
C20H22N2O2
CAS Number:
Molecular Weight:
322.40
UNSPSC Code:
12352200
NACRES:
NA.77
$128.25
List Price$135.00Save 5%Web-Only Promotion
Available to ship onApril 28, 2025Details
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assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
CC1=CC=C(NC(CNCCCOC2=CC=CC=C2)=CC3=O)C3=C1
Related Categories
Biochem/physiol Actions
Selective, high-affinity dopamine D4 receptor (DRD4) partial agonist with a 7.4-fold bias toward arrestin recruitment over Gα signaling with respect to quinpirole.
UCSF924 (Compound 9-6-24; ZINC000091726127) is a selective, high-affinity dopamine D4 receptor (DRD4) partial agonist (Ki = 3 nM for human D4) with a 7.4-fold bias toward arrestin recruitment over Gαi (Gαi/0; Gi/G0) signaling activation with respect to quinpirole. UCSF924 exhibits no detectable affinity for D2, D3 or the F261V/L328F D4 mutant and no agonist activity toward a panel of 320 nonolfactory GPCRs even at a high concentration of 1 μM. The UCSF924 structure analog UCSF924NC (Comound 9-6-16; ZINC000091707446) is the recommended negative control compound with a 1/2500-fold reduced D4 affinity.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Sheng Wang et al.
Science (New York, N.Y.), 358(6361), 381-386 (2017-10-21)
Dopamine receptors are implicated in the pathogenesis and treatment of nearly every neuropsychiatric disorder. Although thousands of drugs interact with these receptors, our molecular understanding of dopaminergic drug selectivity and design remains clouded. To illuminate dopamine receptor structure, function, and
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Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human
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Neurobiology of disease, 103, 11-23 (2017-04-01)
Neurogenesis impairment is considered a major determinant of the intellectual disability that characterizes Down syndrome (DS), a genetic condition caused by triplication of chromosome 21. Previous evidence obtained in the Ts65Dn mouse model of DS showed that the triplicated gene
Kevin Quinn et al.
Journal of pharmaceutical sciences, 101(4), 1462-1474 (2012-01-04)
ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability, suggesting it is a Biopharmaceutics Classification System Class II compound. The poor absolute
Inger Lauritzen et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 32(46), 16243-1655a-16243-1655a (2012-11-16)
Triple-transgenic mice (3xTgAD) overexpressing Swedish-mutated β-amyloid precursor protein (βAPP(swe)), P310L-Tau (Tau(P301L)), and physiological levels of M146V-presenilin-1 (PS1(M146V)) display extracellular amyloid-β peptides (Aβ) deposits and Tau tangles. More disputed is the observation that these mice accumulate intraneuronal Aβ that has been
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