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Search Results for " monoacylglycerol lipase "

34

抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T9687 MAGL-IN-4

His121 ARG57

Lipase Metabolism
MAGL-IN-4 (His121 ARG57) 是选择性的、口服有效的、可透过血脑屏障的、可逆的单酰基甘油脂肪酶抑制剂,IC50=6.2 nM。它主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油水平来增强内源性大麻素信号。
T15632 JW 642

Lipase Metabolism
JW 642 是一种高效的MAGL 抑制剂,对小鼠、大鼠和人源脑细胞膜上MAGL 的IC50值分别为7.6nM、14nM 和3.7nM。
T15635 JZP-430

Lipase; MAGL Metabolism
JZP-430 是不可逆的、高度选择性的 α/β 水解酶结构域 6 抑制剂,能够靶向抑制人类 ABHD6 ,其 IC50=44 nM。
T17260 WWL70

Lipase; MAGL Metabolism
WWL70 是选择性 α/β 水解酶结构域 6 抑制剂,其IC50=70 nM。
T15614 JJKK 048

Lipase Metabolism
JJKK 048 是一种有效的特异性 MAGL 抑制剂。
T5353 ABX-1431

Elcubragistat

Lipase Metabolism
ABX-1431 (Elcubragistat) 是口服具有活力的、选择性CNS-渗透性单酰基甘油脂肪酶抑制剂,IC50=14 nM。
T8974 ML-211

Others Others
ML-211 是基于氨基甲酸酯的酰基蛋白硫酯酶1 / 溶血磷脂酶1 (IC50=17 nM) 和LYPLA2(IC50=30 nM) 的双重抑制剂。它能够抑制丝氨酸水解酶ABHD11 (IC50=10 nM),但在 20 个丝氨酸水解酶组合中,对 LYPLA 的选择性为 50 倍。
T9967 MAGL-IN-5

Lipid Metabolism
MAGL-IN-5 是一种非选择性脂肪酶抑制剂。
T4052 KML29

Lipase Metabolism
KML29 是一种口服具有活性的、高度选择性的不可逆 MAGL 抑制剂,其对小鼠、大鼠和人的 IC50值分别为15 nM、43 nM 和 5.9 nM。它对 FAAH 在内的其他中心和外周丝氨酸水解酶的交叉反应极小。
T5815 MJN110

Cravatt Reagent

Lipase Metabolism
MJN110 (Cravatt Reagent) 是选择性的、口服具有活性的单酰基甘油脂肪酶 (MAGL) 抑制剂,对 hMAGL 和 2-花生四烯酸甘油酯 (2-AG) 的IC50分别为 9.1 nM 和 2.1 nM。它具有阿片类药物保护作用,具有显著的抗痛觉过敏活性。
T8994 ML-​226

ML226,ML-226

MAGL Metabolism
ML226 是 α/β hydrolase domain-containing protein 11 抑制剂,体外和原位的 IC50s 分别为 15 和 0.68 nM。
T2338 JZL195

FAAH; Lipase; Autophagy Autophagy; Metabolism; Neuroscience
JZL195 是一种选择性有效的脂肪酸酰胺水解酶和单酰甘油脂肪酶双重抑制剂,IC50s 分别为 2 和 4 nM。
T6554 JZL 184

JZL184

Lipase Metabolism
JZL 184 是不可逆的、选择性的MAGL 抑制剂,对MAGL 的选择性比 FAAH 高 300 倍以上。它可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50为 8 nM)。
T61294 Monoacylglycerol lipase inhibitor 1

Monoacylglycerol lipase inhibitor 1 是一种有效的单酰基甘油脂肪酶 (MGL) 抑制剂 (化合物 13)。
T9374 AA38-3

1-Piperidinecarboxylic acid, 4-nitrophenyl ester

FAAH; Lipase; MAGL Metabolism; Neuroscience
AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) 是丝氨酸水解酶抑制剂,能够抑制三种 SHs:ABHD6,ABHD11 和 FAAH。
T11724 JNJ-42226314

Lipase Metabolism
JNJ-42226314 是一种具有高选择性的非共价单酰基甘油脂肪酶 (MAGL) 抑制剂,具有抗伤害作用。JNJ-42226314 通过内源性大麻素-2-丙烯酰甘油(2-AG)在神经病理性疼痛和炎症性疼痛模型中显示出疗效。
T27405 GAT211

GAT-211,AZ-4,GAT 211,AZ 4,AZ4

GAT211 is a CB1 positive allosteric modulator. GAT211 suppresses allodynia and produces synergistic antiallodynic effects with monoacylglycerol lipase and fatty acid amide hydrolase inhibitors in paclitaxel-treated mice.
T3591 URB602

Lipase; Antibacterial Metabolism; Microbiology/Virology
URB602 是选择性单酰基甘油脂肪酶 (MGL) 抑制剂,非竞争性抑制大鼠脑 MGL,IC50为 28±4 μM。
T28165 NF-1819

NF 1819,NF1819

Lipase Metabolism
NF-1819 是一种高效、选择性的不可逆 MGL (β-内酰胺基单酰甘油脂肪酶)抑制剂。NF-1819 在体内多发性硬化症模型中缓解疾病症状,在体内急性炎性疼痛模型中表现出镇痛作用。NF-1819 具有较高的膜通透性和血脑屏障通透性。
T71493 AM6580

AM6580 is an irreversible monoacylglycerol lipase (MGL) inhibitor.
T11939 MAGL-IN-1

Lipase Metabolism
MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.
T27811 LEI-106

LEI-106, a novel potent sn-1 DAGLalpha inhibitor, blocks the hydrolysis of sn-1-oleoyl-2-AG, inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6.
T35786 O-7460

In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-depe...
T36498 CAY10762

CAY10762

CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50= 34.1 nM).1It reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells when used at a concentration of 1 μM. CAY10762 (10 mg/kg) increases levels of 2-arachidonoyl glycerol in mouse brain. 1.Castelli, R., Scalvini, L., Vacondio, F., et al.Benzisothiazolinone derivatives as potent allosteric monoacylglycerol lipase inhibitors that functionally mimic sulfenylation of regulatory cysteinesJ. Med. Chem.63(...
T81880 MAGL-IN-11

MAGL Metabolism
MAGL-IN-11(化合物 29),一种选择性且可逆的MAGL抑制剂,具备研究炎症、癌症和抗氧化潜力。
T21905 N-Arachidonyl Maleimide

N-Arachidonyl maleimide 是一种有效且不可逆的单酰基甘油脂肪酶 (MAGL) 抑制剂,IC50值为 140 nM。
T61198 FAAH/MAGL-IN-1

FAAH/MAGL-IN-1, also known as compound SIH 3, is a highly effective inhibitor of FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase). It exhibits IC50 values of 31 nM and 29 nM against FAAH and MAGL, respectively. This compound shows promising potential for advancing research in the field of neuropathic pain [1].
T81879 MAGL-IN-8

MAGL Metabolism
MAGL-IN-8 (compound 13) 是一种针对 hMAGL 的高选择性可逆抑制剂,其IC50值为2.5 ± 0.4 nM。
T81878 MAGL-IN-9

MAGL Metabolism
MAGL-IN-9 (compound 16)为高选择性、可逆MAGL抑制剂,其IC50值为2.7 nM[1]< /sup >。
T81881 MAGL-IN-10

MAGL Metabolism
MAGL-IN-10为一种可逆MAGL抑制剂,展现出优良的ADME特性且体内毒性低。该化合物适用于癌症、神经系统疾病和炎症病理学研究。
T62671 FAAH/MAGL-IN-3

FAAH/MAGL-IN-3 (Compound 10) 是一种不可逆的脂肪酸酰胺水解酶 (FAAH)和单酰基甘油脂酶 (MAGL)双重抑制剂,能够作用于 FAAH (IC50: 179 nM) 和 MAGL (IC50: 759 nM)。FAAH/MAGL-IN-3 表现出很小的 PAMPA (平行人工膜渗透性试验) 透过性。
T73317 JZP-MA-13

JZP-MA-13是一种选择性α/β-水解酶结构域6 (ABHD6) 抑制剂,其IC50值为392 nM。该化合物对MAGL、ABHD12、FAAH或其它丝氨酸水解酶不表现出抑制作用。JZP-MA-13还被用作ABHD6在体内成像的正电子发射断层扫描(PET)配体。
T37629 IDFP

The endocannabinoids, 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA), are biologically active lipids that regulate diverse neurological and metabolic functions by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) hydrolyze 2-AG and AEA, respectively, thus terminating their biological function. IDFP is an organophosphorus compound that dually inhibits MAGL and F...
T37374 URB754

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fa...

化合物

MAGL-IN-4
Cat.No: T9687
Synonym: His121 ARG57
Target: Lipase
JW 642
Cat.No: T15632
Synonym:
Target: Lipase
JZP-430
Cat.No: T15635
Synonym:
Target: Lipase, MAGL
WWL70
Cat.No: T17260
Synonym:
Target: Lipase, MAGL
JJKK 048
Cat.No: T15614
Synonym:
Target: Lipase
ABX-1431
Cat.No: T5353
Synonym: Elcubragistat
Target: Lipase
ML-211
Cat.No: T8974
Synonym:
Target: Others
MAGL-IN-5
Cat.No: T9967
Synonym:
Target: Lipid
KML29
Cat.No: T4052
Synonym:
Target: Lipase
MJN110
Cat.No: T5815
Synonym: Cravatt Reagent
Target: Lipase
ML-​226
Cat.No: T8994
Synonym: ML226,ML-226
Target: MAGL
JZL195
Cat.No: T2338
Synonym:
Target: FAAH, Lipase, Autophagy
JZL 184
Cat.No: T6554
Synonym: JZL184
Target: Lipase
Monoacylglycerol lipase inhibitor 1
Cat.No: T61294
Synonym:
Target:
AA38-3
Cat.No: T9374
Synonym: 1-Piperidinecarboxylic acid, 4-nitrophenyl ester
Target: FAAH, Lipase, MAGL
JNJ-42226314
Cat.No: T11724
Synonym:
Target: Lipase
GAT211
Cat.No: T27405
Synonym: GAT-211,AZ-4,GAT 211,AZ 4,AZ4
Target:
URB602
Cat.No: T3591
Synonym:
Target: Lipase, Antibacterial
NF-1819
Cat.No: T28165
Synonym: NF 1819,NF1819
Target: Lipase
AM6580
Cat.No: T71493
Synonym:
Target:
MAGL-IN-1
Cat.No: T11939
Synonym:
Target: Lipase
LEI-106
Cat.No: T27811
Synonym:
Target:
O-7460
Cat.No: T35786
Synonym:
Target:
CAY10762
Cat.No: T36498
Synonym: CAY10762
Target:
MAGL-IN-11
Cat.No: T81880
Synonym:
Target: MAGL
N-Arachidonyl Maleimide
Cat.No: T21905
Synonym:
Target:
FAAH/MAGL-IN-1
Cat.No: T61198
Synonym:
Target:
MAGL-IN-8
Cat.No: T81879
Synonym:
Target: MAGL
MAGL-IN-9
Cat.No: T81878
Synonym:
Target: MAGL
MAGL-IN-10
Cat.No: T81881
Synonym:
Target: MAGL
FAAH/MAGL-IN-3
Cat.No: T62671
Synonym:
Target:
JZP-MA-13
Cat.No: T73317
Synonym:
Target:
IDFP
Cat.No: T37629
Synonym:
Target:
URB754
Cat.No: T37374
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5737 euphol

Others; Lipase; Endogenous Metabolite Metabolism; Others
Euphol 是从Euphorbia tirucalli 的汁液中分离出来的四环三萜醇,具有抗炎和免疫调节作用,口服具有活力。 它通过能够逆机制抑制单酰基甘油脂肪酶 (MGL) 的特性,IC50=315 nM。 外周 MGL 抑制能够调节内源性大麻素系统从而阻止炎症性疼痛的发展。

天然产物

euphol
Cat.No: T5737
Synonym:
Target: Others, Lipase, Endogenous Metabolite
TargetMol Loading
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