SML2714
VU0155072
≥98% (HPLC)
别名:
N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)-2-naphthamide, N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)naphthalene-2-carboxamide, N-[2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-8-yl)ethyl]-2-naphthalenecarboxamide, NOPT, VU0155072-2
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About This Item
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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
InChI
1S/C26H28N4O2/c31-24(22-11-10-20-6-4-5-7-21(20)18-22)27-14-17-29-15-12-26(13-16-29)25(32)28-19-30(26)23-8-2-1-3-9-23/h1-11,18H,12-17,19H2,(H,27,31)(H,28,32)
InChI 密鑰
FAIFAFUXFFWVNQ-UHFFFAOYSA-N
生化／生理作用
VU0155072 is a PLD2-selective, PH domain-targeting allosteric phospholipase D inhibitor (human PLD2/PLD1 IC50 = 140 nM/5.1 μM vs. PH/PX-deleted rat PLD1 IC50 >20 μM; cellular PLD IC50 = 110 nM/GFP-PLD2-overexpressing HEK293 vs. 1 μM/PMA-stimulated Calu-1 with predominant PLD1 activity) that selectively suppresses PLD2-dependent MDA-MB-231 invasion in cultures (by 60% in 48 hrs; 200 nM) and exhibits in vivo efficacy in murine models of DSS-induced colitis (4 mg/kg/day p.o.) and breast tumor-associated macrophages/neutrophils infiltration (75 μg/0.11 μL/kg/hr via osmotic pump). Use low concentrations (<5 μM) for cell treatment to avoid dual PLD1/2 inhibition.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Najwa Skafi et al.
Journal of cellular physiology, 234(4), 4825-4839 (2018-09-13)
Vascular calcification (VC) is the pathological accumulation of calcium phosphate crystals in one of the layers of blood vessels, leading to loss of elasticity and causing severe calcification in vessels. Medial calcification is mostly seen in patients with chronic kidney
Anusha Mishra et al.
Nature neuroscience, 19(12), 1619-1627 (2016-11-01)
Active neurons increase their energy supply by dilating nearby arterioles and capillaries. This neurovascular coupling underlies blood oxygen level-dependent functional imaging signals, but its mechanism is controversial. Canonically, neurons release glutamate to activate metabotropic glutamate receptor 5 (mGluR5) on astrocytes
José R Fernández et al.
Archives of dermatological research, 309(2), 103-110 (2016-12-19)
Isoprenylcysteine (IPC) small molecules were discovered as signal transduction modulating compounds ~25 years ago. More recently, IPC molecules have demonstrated antioxidant and anti-inflammatory properties in a variety of dermal cells as well as antimicrobial activity, representing a novel class of compounds
Guangxi Zhou et al.
Mediators of inflammation, 2016, 2543070-2543070 (2016-10-11)
Background. Inflammatory bowel diseases (IBD), including Crohn's disease (CD) and ulcerative colitis (UC), are chronically remittent and progressive inflammatory disorders. Phospholipase D2 (PLD2) is reported to be involved in the pathogenesis of several inflammatory diseases. However, the exact role of
Shuwei Xie et al.
Molecular biology of the cell, 27(1), 108-126 (2015-10-30)
The endocytic recycling compartment (ERC) is a series of perinuclear tubular and vesicular membranes that regulates recycling to the plasma membrane. Despite evidence that cargo is sorted at the early/sorting endosome (SE), whether cargo mixes downstream at the ERC or
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