SML3379
D159687
≥98% (HPLC)
别名:
1-(4-((3′-Chloro-6-methoxy-[1,1′-biphenyl]-3-yl)methyl)phenyl)urea, D 159687, N-[4-[(3′-Chloro-6-methoxy[1,1′-biphenyl]-3-yl)methyl]phenyl]urea, [4-(3′-Chloro-6-methoxy-biphenyl-3-ylmethyl)phenyl]urea, [4-[[3-(3-Chlorophenyl)-4-methoxyphenyl]methyl]phenyl]urea
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About This Item
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![1H-[1,2,4]恶二唑并[4,3-a]喹恶啉-1-酮 powder](/deepweb/assets/sigmaaldrich/product/structures/764/715/605dc5a5-0864-471b-a71e-bd2aa6553c1d/640/605dc5a5-0864-471b-a71e-bd2aa6553c1d.png)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (Warmed)
储存温度
2-8°C
SMILES字符串
Clc1cc(ccc1)c2c(ccc(c2)Cc3ccc(cc3)NC(=O)N)OC
InChI
1S/C21H19ClN2O2/c1-26-20-10-7-15(12-19(20)16-3-2-4-17(22)13-16)11-14-5-8-18(9-6-14)24-21(23)25/h2-10,12-13H,11H2,1H3,(H3,23,24,25)
InChI key
RJJLUTWHJUDZFP-UHFFFAOYSA-N
生化/生理作用
D159687 is a brain-penetrant, orally available, highly potent and selective negative allosteric modulator (NAM) against phosphodiesterase 4 (PDE4) subtype PDE4D (hPDE4D7 IC50 = 27 nM; PDE4A1/B1/C1 IC50 = 2.50/1.47/6.80 μM; IC50 ≥29 μM against PDE1/2/3/5/7/8/9/10/11 subtypes). Comparing to Rolipram, D159678 offers similar in vivo efficacy on long-term memory formation by novel object recognition test (MED = 3 μg/kg mouse iv., 1 μg/kg rat p.o.), while being more effective in the scopolamine-impaired Y-maze tests (D159678/Rolipram MED = 0.1/1 μg/kg mouse iv. or 30/100 μg/kg mouse p.o.) and much less emetic in shrews/dog/monkeys (by 100-/3000-/500-fold).
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
从最新的版本中选择一种：
分析证书(COA)
Lot/Batch Number
David J Titus et al.
Neurobiology of learning and memory, 148, 38-49 (2018-01-03)
Traumatic brain injury (TBI) significantly decreases cyclic AMP (cAMP) signaling which produces long-term synaptic plasticity deficits and chronic learning and memory impairments. Phosphodiesterase 4 (PDE4) is a major family of cAMP hydrolyzing enzymes in the brain and of the four
Jane S Sutcliffe et al.
PloS one, 9(7), e102449-e102449 (2014-07-23)
Cyclic adenosine monophosphate (cAMP) signalling plays an important role in synaptic plasticity and information processing in the hippocampal and basal ganglia systems. The augmentation of cAMP signalling through the selective inhibition of phosphodiesterases represents a viable strategy to treat disorders
Alex B Burgin et al.
Nature biotechnology, 28(1), 63-70 (2009-12-29)
Phosphodiesterase 4 (PDE4), the primary cAMP-hydrolyzing enzyme in cells, is a promising drug target for a wide range of conditions. Here we present seven co-crystal structures of PDE4 and bound inhibitors that show the regulatory domain closed across the active
Chong Zhang et al.
Scientific reports, 7, 40115-40115 (2017-01-06)
Inhibition of cyclic AMP (cAMP)-specific phosphodiesterase 4 (PDE4) has been proposed as a potential treatment for a series of neuropsychological conditions such as depression, anxiety and memory loss. However, the specific involvement of each of the PDE4 subtypes (PDE4A, 4B
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