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Cat. No. | Product Name | Target | Signaling Pathways |
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T61294 |
Monoacylglycerol lipase inhibitor 1
|
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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)。 | |||
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。 | |||
T15614 |
JJKK 048
|
Lipase | Metabolism |
JJKK 048 是一种有效的特异性 MAGL 抑制剂。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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)。 | |||
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。 | |||
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。 | |||
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。 | |||
T27405 |
GAT211
GAT-211,AZ-4,GAT 211,AZ 4,AZ4 |
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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. | |||
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。 | |||
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。 | |||
T36454 |
1-Stearoyl-rac-glycerol
|
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1-Stearoyl-rac-glycerol is a monoacylglycerol that contains stearic acid at the sn-1 position. 1-Stearoyl-rac-glycerol levels are decreased in tumor tissue in a mouse model of azoxymethane-induced colorectal carcinogenesis. Levels of 1-stearoyl-rac-glycerol are decreased in lung tissue from patients with adenocarcinoma, but are increased in the serum of patients with Buruli ulcer and in the cerebrospinal fluid of patients with the inflammatory demyelinating diseases multiple sclerosis (MS), neur... | |||
T12028 | MGAT2-IN-1 | Others | Others |
MGAT2-IN-1 is an orally active monoacylglycerol acyltransferase (MGAT2)inhibitor (human and mouse MGAT2 with IC50 of 7.8 and 2.4 nM , respectively). | |||
T11939 |
MAGL-IN-1
|
Lipase | Metabolism |
MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM. | |||
T71493 |
AM6580
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AM6580 is an irreversible monoacylglycerol lipase (MGL) inhibitor. | |||
T16494 |
PF-06471553
|
Others | Others |
PF-06471553 is an effective and selective inhibitor of monoacylglycerol acyltransferase 3 (IC50: 92 nM). | |||
T37281 |
1-Palmitoleoyl glycerol
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1-Palmitoleoyl glycerol 是具有生物活性的单酰基甘油,在 Caco-2 细胞中可抑制 P-糖蛋白,还能诱导胸腺细胞凋亡。 | |||
T27811 |
LEI-106
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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. | |||
T36498 |
CAY10762
CAY10762 |
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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(... | |||
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]. | |||
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。 | |||
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。 | |||
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。 | |||
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 >。 | |||
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。 | |||
T81802 |
MGAT2-IN-4
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MGAT2-IN-4(compound 33)是一种针对单酰基甘油转移酶2(MGAT2)的抑制剂,显示出良好的肝脏代谢稳定性,适用于肥胖症、糖尿病以及非酒精性脂肪性肝炎(NASH)的研究。 | |||
T35786 |
O-7460
|
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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... | |||
T35444 |
1-Pentadecanoyl-rac-glycerol
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1-Pentadecanoyl-rac-glycerol is a monoacylglycerol that contains pentadecanoic acid at the sn-1 position. It has been found in wheat bran extracts.1 1-Pentadecanoyl-rac-glycerol levels are increased in a HepaRG cell-based model of hepatic steatosis induced by BSA-conjugated palmitate.2 |1. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).|2. Brown, M.V., Compton, S.A., Milburn, M... | |||
T37286 |
1-Undecanoyl-rac-glycerol
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1-Undecanoyl-rac-glycerol is a monoacylglycerol that contains undecanoic acid at the sn-1 position. It completely inhibits the growth of the bacteria B. cereus, B. subtilis, M. luteus, E. faecalis, and S. aureus when used at concentrations ranging from 250 to 1,500 mg/L.1 1-Undecanoyl-rac-glycerol (0.1 and 0.3 mg/ml) also has antifungal activity against K. marxianus, S. cerevisiae, and C. maltosa.2 | |||
T37887 |
1-Heptadecanoyl-rac-glycerol
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1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg/ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3 |1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. ... | |||
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。 | |||
T37629 |
IDFP
|
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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... | |||
T73317 |
JZP-MA-13
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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。 | |||
T37374 |
URB754
|
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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... | |||
T37691 |
Phosphatidic Acids (egg) (ammonium salt)
|
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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 ... | |||
T35445 |
1-Stearoyl-3-Oleoyl-rac-glycerol
|
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1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fa... |
Cat. No. | Product Name | Target | Signaling Pathways |
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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。 | |||
TN7251 |
Olivetol Dimethyl Ether
1,3-dimethoxy-5-pentylbenzene |
Others | Others |
Olivetol Dimethyl Ether 是一种单酰基甘油,具有镇痛活性和潜在的抗炎活性,可以抑制脂肪酸的合成。 |