Cat. No. | Product Name | Target | Signaling Pathways |
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T15268 |
FAAH-IN-2
O-Desmorpholinopropyl Gefitinib,4-(3-氯-4-氟苯氨基)-7-甲氧基喹唑啉-6-醇 |
FAAH; Autophagy | Autophagy; Metabolism; Neuroscience |
FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) 是一种脂肪酸酰胺水解酶的有效抑制剂。 | |||
T61707 |
FAAH/MAGL-IN-2
|
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FAAH/MAGL-IN-2 是一种有效的,可逆的,具有口服活性且可透过血脑屏障的 FAAH 和 MAGL 抑制剂,其IC50值分别为 11 nM 和 36 nM (b>Ki 值分别为 28 nM 和 60 nM)。FAAH/MAGL-IN-2 有研究神经性疼痛的潜力而不引起运动障碍。 | |||
T67745 |
CB2R/FAAH modulator-2
|
Cannabinoid Receptor; FAAH | GPCR/G Protein; Metabolism; Neuroscience |
CB2R/FAAH modulator-2 (compound 26) 是一种双重靶点的调节剂,是 CB2R 的激动剂,也是 FAAH 的抑制剂,作用于 CB2R 和 CB1R 的 Ki 值分别是 10.8 和 152.9 nM,作用于FAAH 的 IC50 值为 6.2 μM。CB2R/FAAH modulator-2 可用于癌症、神经退行性疾病中发生的有害炎症级联反应以及 COVID-19 感染相关研究。 | |||
T67896 |
CB2R/FAAH modulator-1
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Cannabinoid Receptor; FAAH | GPCR/G Protein; Metabolism; Neuroscience |
CB2R/FAAH modulator-1是一种大麻素2型受体(CB2R)激动剂,同时也是脂肪酸酰胺水解酶(FAAH)抑制剂(IC50=4 μM),可减少促炎和增加抗炎细胞因子的产生,常用于炎症研究。对 CB2R 和 CB1R 的Kis 分别为14.8 nM 和241.3 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)。 | |||
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。 | |||
T38223 |
N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide
|
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N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide binds to the cannabinoid 1 (CB1) receptor with a Ki value of 365 nM in a radioligand binding assay using rat brain homogenate. It has an EC50 value of 698 nM for the peroxisome proliferator-activated receptor α (PPARα) in a luciferase reporter assay and, in rats, it decreases food intake. It does not inhibit fatty acid amide hydrolase (FAAH). | |||
T38138 |
ACEA
2'-chloro-AEA,Arachidonoyl 2'-Chloroethylamide |
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Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in ... | |||
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... | |||
T37684 |
CAY10412
CAY10412 |
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Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system. AEA undergoes reuptake into neurons by a facilitated process. Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH). CAY10412 is an analog of AEA that has no intrinsic binding affinity for... | |||
T70882 |
Orlistat-d3
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Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit... |