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31

抑制剂 & 化合物

9

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Cat. No. Product Name Target Signaling Pathways
T11037 Diacylglycerol acyltransferase inhibitor-1

Others Others
Diacylglycerol Acyltransferase Inhibitor-1, a diacylglycerol acyltransferase (DGAT1) inhibitor, effectively suppresses the activity of DGAT1.
T13373 YM17E

Acyltransferase; AChR Metabolism; Neuroscience
YM17E 是一种 ACAT 抑制剂,在体外兔肝微粒体中的 IC50 为 44 nM。
T9711 OGT-IN-2

Others Others
OGT-IN-2 是 OGT 抑制剂,抑制 sOGT 和 ncOGT 的 IC50分别为 30 μM 和 53 μM。它在关节疾病方面有研究的价值,如关节软骨疾病、骨关节炎。
T12767 RP 70676

Acyltransferase Metabolism
RP 70676 是ACAT 抑制剂,抑制大鼠和兔子中 ACAT 的IC50分别为 25 和 44 nM。
T15109 DGAT1-IN-1

Transferase Metabolism
DGAT1-IN-1是 DGAT1的高效抑制剂,在 Hep3B 细胞过表达 DGAT1裂解物中,测得IC50低于10nM。
T8236 RHC 80267

U-57908

Others; Phospholipase; COX; Acyltransferase; AChR Immunology/Inflammation; Metabolism; Neuroscience; Others
RHC 80267 (U-57908) 是一种选择性二酰基甘油脂酶(DAGL)抑制剂,对犬血小板的IC50为 4 μM。它抑制COX 活性和磷脂酰胆碱的水解,还抑制胆碱酯酶活性,IC50为 4 μM,增强乙酰胆碱引起的松弛。
T23550 YM-750

YM 750

Acyltransferase Metabolism
YM-750 是一种有效的酰基:胆固醇酰基转移酶(ACAT)抑制剂,IC50为0.18 μM。
T16409 OSMI-1

Others; Acyltransferase Metabolism; Others
OSMI-1 是一种 O-GlcNAc 转移酶 (OGT) 抑制剂 (IC50=2.7 μM),具有口服活性和细胞渗透性。OSMI-1 可以抑制蛋白质 O-GlcNA 酰化,而不会定性地改变细胞表面 N- 或 O- 连接的聚糖。
T11733 K-604 dihydrochloride

Acyltransferase Metabolism
K-604 dihydrochloride 是酰基辅酶 A:胆固醇酰基转移酶 1 的选择性抑制剂,IC50为 0.45±0.06 μM。
T8314 RP-64477

RP64477

Acyltransferase Metabolism
RP-64477 是有效的胆固醇酯化酶酰基辅酶 A:胆固醇 O-酰基转移酶 (ACAT) 抑制剂。
T23521 VULM 1457

Acyltransferase Metabolism
VULM 1457 是有效的胆固醇酰基转移酶抑制剂,具有显著的降血脂活性,并改善了整体心肌缺血再灌注损伤结果。VULM 1457 显著降低肾上腺髓质素的产生和分泌,并下调人肝母细胞上的 AM 受体。VULM 1457 具有研究糖尿病和高胆固醇血症的潜力。
T10035 10,12-Tricosadiynoic acid

TDA,TCDA

Acyltransferase Metabolism
10,12-Tricosadiynoic acid 是一种口服有效的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂,具有高特异性,选择性,高亲和力的特点。10,12-Tricosadiynoic acid 可改善线粒体脂质和 ROS 代谢,在高脂饮食或肥胖引起的代谢性疾病中有研究的价值。
T12425 PF-06424439 methanesulfonate

Acyltransferase; Transferase Metabolism
PF-06424439 methanesulfonate 是一种口服有效咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂,IC50是14 nM。PF-06424439 methanesulfonate 具有缓慢可逆,时间依赖性的特点,其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。
T6937 PF-04620110

PF04620110,PF 04620110

Acyltransferase; Transferase Metabolism
PF-04620110 是一种口服有效的甘油二酯酰基转移酶 -1(DGAT1)选择性抑制剂,IC50为 19 nM。
T22665 PD 128042

CI 976

Acyltransferase Metabolism
PD 128042 (CI 976) 是口服有效的ACAT (酰基辅酶 A: 胆固醇酰基转移酶)选择性抑制剂。它也是LPAT(溶血磷脂酰基转移酶) 抑制剂。它抑制高尔基体相关 LPAT 活性 (IC50=15 μM)。它抑制多种膜运输步骤,包括在内吞和分泌途径中发现的步骤。
T4681 T863

DGAT-3,DGAT-1 inhibitor

Acyltransferase; Transferase Metabolism
T863 (DGAT-3) 是口服有效的二酰基甘油酰基转移酶1 选择性抑制剂。T863结合DGAT1的酰基辅酶A 结合位点,抑制三酰甘油在细胞内的合成。
T2753 Avasimibe

PD-148515,阿伐麦布,CI-1011

P450; Acyltransferase Metabolism
Avasimibe (PD-148515) 是一种口服有效的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂,对 ACAT1和 ACAT2的 IC50分别为 24 和 9.2 µM。Avasimibe 在前列腺癌中有研究的价值。
T12225L Nevanimibe hydrochloride

PD-132301 hydrochloride,ATR101 hydrochloride

Apoptosis; Acyltransferase Apoptosis; Metabolism
Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的,选择性酰基辅酶 A:胆固醇 O-酰基转移酶 1 抑制剂,EC50为 9 nM。它抑制 ACAT2,EC50为 368 nM。它诱导细胞凋亡,具有抗肾上腺皮质癌的潜力。
T15247 ESI-05

NSC 116966

cAMP GPCR/G Protein
ESI-05 (NSC-116966) 是特异性的 cAMP 直接激活交换蛋白 2 (EPAC2) 拮抗剂(IC50:0.4 µM),能够抑制 cAMP 诱导的 EPAC2 的活化,并 EAPC2 介导的 Rap1 的活化。
T6365 A 922500

A922500,(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸,DGAT-1 Inhibitor 4a

Acyltransferase; Transferase Metabolism
A 922500 (DGAT-1 Inhibitor 4a) 是一种口服有效的二酰甘油酰基转移酶 1(DGAT-1)选择性抑制剂,抑制小鼠和人 DGAT-1 的IC50s 分别为9 nM,22 nM。
T12426 PF-06424439

Acyltransferase; Transferase Metabolism
PF-06424439 是一种口服有效的咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂,IC50是 14 nM。PF-06424439 具有缓慢可逆的,时间依赖性的特点,其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。
T9186 Ervogastat

PF-06865571

Transferase Metabolism
Ervogastat (PF-06865571) 是一种有效且耐受性良好的二酰基甘油酰基转移酶 2 抑制剂。 Ervogastat 可降低非酒精性脂肪性肝炎 (NASH) 中的脂肪变性和肝脏甘油三酯水平。
T11827 Pradigastat

ANJ908,LCQ908-NXA,LCQ908A,LCQ-908

Transferase Metabolism
Pradigastat (LCQ-908) 是一种具有口服活性、有效性和选择性的二酰基甘油酰基转移酶 1 (DGAT1) 抑制剂,可用于治疗便秘,可用于研究肥胖和糖尿病。
T11016 DGAT-1 inhibitor 2

Transferase Metabolism
DGAT-1 inhibitor 2是有效的DGAT-1抑制剂,具有减肥功效。
T24128 H2-005

H2 005

H2-005 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
T27692 JNJ-DGAT2-B

JNJDGAT2B,JNJ DGAT2 B

JNJ-DGAT2-B is a selective inhibitor of Diacylglycerol acyltransferase 2.
T24127 H2-003

H2003

H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
T70160 PF-06427878

PF-06427878 is an orally active, potent and selective diacylglycerol acyltransferase 2 inhibitor.
T79764 PF-07202954

Acyltransferase Metabolism
PF-07202954为一种弱碱性DGAT2抑制剂,其对人类DGAT2的IC50值为10 nM。在西方饮食喂养的大鼠模型中,PF-07202954能有效降低肝脏内的甘油三酯含量。
T71886 ALN29882

ALN29882 is a glycerolipid, that is located at the plasma membrane. It is made up of two fatty acid chains that are covalently attached to a single glycerol molecule with the help of an ester linkage. 18:1 DG has been used as a diacyl-glycerol source in diacylglycerol O-acyltransferase 1 (DGAT1) assay. It has also been used as substrate to assess compounds as potential inhibitors of DGAT-1 in DGAT-1 enzyme assay. It is suitable to use in lipid-protein overlay screen assay with the recombinant p...
T37691 Phosphatidic Acids (egg) (ammonium salt)

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular ...

化合物

Diacylglycerol acyltransferase inhibitor-1
Cat.No: T11037
Synonym:
Target: Others
YM17E
Cat.No: T13373
Synonym:
Target: Acyltransferase, AChR
OGT-IN-2
Cat.No: T9711
Synonym:
Target: Others
RP 70676
Cat.No: T12767
Synonym:
Target: Acyltransferase
DGAT1-IN-1
Cat.No: T15109
Synonym:
Target: Transferase
RHC 80267
Cat.No: T8236
Synonym: U-57908
Target: Others, Phospholipase, COX, Acyltransferase, AChR
YM-750
Cat.No: T23550
Synonym: YM 750
Target: Acyltransferase
OSMI-1
Cat.No: T16409
Synonym:
Target: Others, Acyltransferase
K-604 dihydrochloride
Cat.No: T11733
Synonym:
Target: Acyltransferase
RP-64477
Cat.No: T8314
Synonym: RP64477
Target: Acyltransferase
VULM 1457
Cat.No: T23521
Synonym:
Target: Acyltransferase
10,12-Tricosadiynoic acid
Cat.No: T10035
Synonym: TDA,TCDA
Target: Acyltransferase
PF-06424439 methanesulfonate
Cat.No: T12425
Synonym:
Target: Acyltransferase, Transferase
PF-04620110
Cat.No: T6937
Synonym: PF04620110,PF 04620110
Target: Acyltransferase, Transferase
PD 128042
Cat.No: T22665
Synonym: CI 976
Target: Acyltransferase
T863
Cat.No: T4681
Synonym: DGAT-3,DGAT-1 inhibitor
Target: Acyltransferase, Transferase
Avasimibe
Cat.No: T2753
Synonym: PD-148515,阿伐麦布,CI-1011
Target: P450, Acyltransferase
Nevanimibe hydrochloride
Cat.No: T12225L
Synonym: PD-132301 hydrochloride,ATR101 hydrochloride
Target: Apoptosis, Acyltransferase
ESI-05
Cat.No: T15247
Synonym: NSC 116966
Target: cAMP
A 922500
Cat.No: T6365
Synonym: A922500,(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸,DGAT-1 Inhibitor 4a
Target: Acyltransferase, Transferase
PF-06424439
Cat.No: T12426
Synonym:
Target: Acyltransferase, Transferase
Ervogastat
Cat.No: T9186
Synonym: PF-06865571
Target: Transferase
Pradigastat
Cat.No: T11827
Synonym: ANJ908,LCQ908-NXA,LCQ908A,LCQ-908
Target: Transferase
DGAT-1 inhibitor 2
Cat.No: T11016
Synonym:
Target: Transferase
H2-005
Cat.No: T24128
Synonym: H2 005
Target:
JNJ-DGAT2-B
Cat.No: T27692
Synonym: JNJDGAT2B,JNJ DGAT2 B
Target:
H2-003
Cat.No: T24127
Synonym: H2003
Target:
PF-06427878
Cat.No: T70160
Synonym:
Target:
PF-07202954
Cat.No: T79764
Synonym:
Target: Acyltransferase
ALN29882
Cat.No: T71886
Synonym:
Target:
Phosphatidic Acids (egg) (ammonium salt)
Cat.No: T37691
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3342 Xanthohumol

Apoptosis; Others; Influenza Virus; COX; Acyltransferase; HSV Apoptosis; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; Others
Xanthohumol 是从啤酒花中分离到的黄酮类化合物,可抑制 COX-1 和 COX-2 活性,具有抗肿瘤,抗血管生成的作用,还具有抗多种病毒的活性。
TN1691 Glabrol

光甘草酚,光甘草醇

P450; NF-κB; NO Synthase; Acyltransferase Immunology/Inflammation; Metabolism; NF-κB
Glabrol 是分离自甘草根的乙醇提取物中的一种异戊二烯类黄酮,是一种有效且非竞争性的酰基辅酶 A:胆固醇酰基转移酶(ACAT)抑制剂,抑制大鼠肝脏微粒体 ACAT 的 IC50为 24.6 μM。
T5544 2-Furoic acid

Furan-2-carboxylic acid,糠酸

Anti-infection; ATP Citrate Lyase; Endogenous Metabolite; Acyltransferase Metabolism; Microbiology/Virology
2-Furoic acid (Furan-2-carboxylic acid) 2-Furoic acid 能够降低血清中胆固醇和甘油三酯的水平,具有抗血脂作用。
T69446 Cochlioquinone A

Cochlioquinone A is an inhibitor of diacylglycerol kinase (DGK) and diacylglycerol acyltransferase (DGAT). It has been shown to reduce the concentration of phosphatidic acid in T cell lymphoma and has also been shown to compete with macrophage inflammatory protein-1α for binding to human CCR5 chemokine receptors.
T37690 Phenylpyropene A

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of ...
TN1843 Kushenol K

PDE; HSV Metabolism; Microbiology/Virology
Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K shows weak antiviral activity against Herpes simplex virus types I and II.
TN3428 Aphadilactone C

Others Others
Aphadilactone C shows significant antimalarial activity with the IC50 value of 170 ± 10 nM. It shows potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 uM, selectivity index > 217).
TN3255 7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone

Others Others
7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone shows diacylglycerol acyltransferase (DGAT)1 inhibition with IC(50) values of 47.0 microM (for rat liver microsomes) and 160.7 microM (for HepG2 cell microsomes),
T75697 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone,为喹诺酮类生物碱,作用为二酰基甘油酰基转移酶抑制剂与血管紧张素II受体阻断剂,其IC50值依次为20.1 μM与34.1 μM。此化合物亦展现对幽门螺杆菌的有效抗活性,MIC值达10 μg/mL。

天然产物

Xanthohumol
Cat.No: T3342
Synonym:
Target: Apoptosis, Others, Influenza Virus, COX, Acyltransferase, HSV
Glabrol
Cat.No: TN1691
Synonym: 光甘草酚,光甘草醇
Target: P450, NF-κB, NO Synthase, Acyltransferase
2-Furoic acid
Cat.No: T5544
Synonym: Furan-2-carboxylic acid,糠酸
Target: Anti-infection, ATP Citrate Lyase, Endogenous Metabolite, Acyltransferase
Cochlioquinone A
Cat.No: T69446
Synonym:
Target:
Phenylpyropene A
Cat.No: T37690
Synonym:
Target:
Kushenol K
Cat.No: TN1843
Synonym:
Target: PDE, HSV
Aphadilactone C
Cat.No: TN3428
Synonym:
Target: Others
7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
Cat.No: TN3255
Synonym:
Target: Others
1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone
Cat.No: T75697
Synonym:
Target:
TargetMol Loading
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