DGAT
TAGs, also termed blood fats, are found in most eukaryotic cells, where they are a mechanism for storing unused calories. They also play an important role in maintaining normal physiology. In eukaryotic cells, TAGs are resynthesized through a reaction catalyzed by diacylglycerol acyltransferase after dietary TAG has been digested and absorbed from by the small intestine as fatty acids and monoacylglycerol. The final and only committed step in the synthesis of TAG is common to both pathways and is catalyzed by acyl-CoA:diacylglycerol acyltransferase (DGAT). This enzyme family is composed of DGAT-1 and DGAT-2, which are encoded by two distinct genes. DGATs have been important molecular tools for examining the relationship between obesity and TAG synthesis. The inhibition of TAG synthesis has been suggested as a method of disrupting lipid absorption in the small intestine, thereby restoring the energy balance through a decrease in energy input; therefore, the inhibition of TAG synthesis in both adipose and non-adipose tissues may be beneficial and a potential therapeutic strategy leading to protection against obesity.
References
1.Naik R,et al. ChemMedChem. 2014 Nov;9(11):2410-24.
References
1.Naik R,et al. ChemMedChem. 2014 Nov;9(11):2410-24.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
DGAT
-
JTT-553 benzosulfonate
产品货号 : M16960
cas no: ——
JTT-553是一种新型有效的选择性DGAT-1抑制剂,IC50为2.38 nM,对人DGAT2和ACA T1没有抑制活性(IC50>10 uM)。 -
DGAT1-IN-4
产品货号 : M16751
cas no: 942999-61-3
一种有效的、选择性的、口服有效的 DGAT-1 抑制剂,对 hDGAT-1 和 mDGAT-1 的 IC50 分别为 15 nM 和 9 nM。 -
JTT-553
产品货号 : M15691
cas no: 701232-94-2
JTT-553 是一种新型有效的选择性 DGAT-1 抑制剂,IC50 为 2.38 nM。 -
PF-04620110
产品货号 : M10407
cas no: 1109276-89-2
PF-04620110 是一种有效的、选择性的、口服生物可利用的 DGAT-1 抑制剂,IC50 为 19 nM,对 DGAT-2 没有活性(IC50>30 uM)。