所有图片(1)
别名:
2-((1,4-trans)-4-(4-(4-Amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)- phenyl)cyclohexyl)acetic acid, T-863, trans-4-[4-(4-Amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-cyclohexaneacetic acid
经验公式（希尔记法）:
C22H26N4O3
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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 15 mg/mL (clear solution)
储存温度
2-8°C
SMILES字符串
CC1(C)Oc2ncnc(N)c2N=C1c3ccc(cc3)[C@@H]4CC[C@H](CC4)CC(O)=O
InChI
1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
InChI key
FUIYMYNYUHVDPT-HDJSIYSDSA-N
应用
T863 has been used as a diglyceride acyltransferase (DGAT1) inhibitor:
- to provide the opportunity to precisely control the DGAT inhibition
- to treat mouse embryonic fibroblasts (MEFs) to analyse lipid droplet biogenesis
- to specifically block neutral lipid synthesis and lipid droplet formation in HT-1080 cells
- to block lipid droplet (LD) formation
生化/生理作用
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
DGAT1-dependent lipid droplet biogenesis protects mitochondrial function during starvation-induced autophagy
Nguyen TB, et al.
Developmental Cell, 42(1), 9-21 (2017)
Angela Castoldi et al.
Nature communications, 11(1), 4107-4107 (2020-08-17)
Foamy macrophages, which have prominent lipid droplets (LDs), are found in a variety of disease states. Toll-like receptor agonists drive triacylglycerol (TG)-rich LD development in macrophages. Here we explore the basis and significance of this process. Our findings indicate that
Jesus A Silvas et al.
bioRxiv : the preprint server for biology (2020-08-04)
Therapeutics targeting replication of SARS coronavirus 2 (SARS-CoV-2) are urgently needed. Coronaviruses rely on host membranes for entry, establishment of replication centers and egress. Compounds targeting cellular membrane biology and lipid biosynthetic pathways have previously shown promise as antivirals and
Lipid droplet formation in Mycobacterium tuberculosis infected macrophages requires IFN gamma/HIF-1alpha signaling and supports host defense
Knight M, et al.
PLoS Pathogens, 14(1), e1006874-e1006874 (2018)
Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state
Magtanong L, et al.
Cell Chemical Biology, 26(3), 420-432 (2019)
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