SML0539
T863
≥98% (HPLC), DGAT1 inhibitor, powder
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
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关于此项目
经验公式（希尔记法）:
C22H26N4O3
化学文摘社编号:
分子量:
394.47
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
T863, ≥98% (HPLC)
SMILES string
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 15 mg/mL (clear solution)
storage temp.
2-8°C
Quality Level
Application
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
Biochem/physiol Actions
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.
T863 is an orally active, selective and potent DGAT1 inhibitor.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state
Magtanong L, et al.
Cell Chemical Biology, 26(3), 420-432 (2019)
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
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)
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
DGAT1-dependent lipid droplet biogenesis protects mitochondrial function during starvation-induced autophagy
Nguyen TB, et al.
Developmental Cell, 42(1), 9-21 (2017)
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