SML2022
UCSF924
≥98% (HPLC)
别名:
6-Methyl-2-((3-phenoxypropylamino)methyl)quinolin-4(1H)-one, ZINC000091726127
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
CC1=CC=C(NC(CNCCCOC2=CC=CC=C2)=CC3=O)C3=C1
生化/生理作用
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
Fiorenza Stagni et al.
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
Gary Probst et al.
Journal of medicinal chemistry, 56(13), 5261-5274 (2013-05-30)
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
Inger Lauritzen et al.
Acta neuropathologica, 132(2), 257-276 (2016-05-04)
Endosomal-autophagic-lysosomal (EAL) dysfunction is an early and prominent neuropathological feature of Alzheimers's disease, yet the exact molecular mechanisms contributing to this pathology remain undefined. By combined biochemical, immunohistochemical and ultrastructural approaches, we demonstrate a link between EAL pathology and the
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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