FAAH
The fatty acid amide hydrolase (FAAH), is the enzyme responsible for the hydrolysis of anandamide, an endocannabinoid. FAAH has broad specificity in terms of other substrates, such as oleamide (a sleep factor) and 2-arachidonoyl glycerol (2- AG), but the significance of these activities in vivo remains to be determined. FAAH is a membrane-bound protein localized predominantly in microsomal or mitochondorial fraction of rat brain and rat liver and porcine brain. The FAAH activity was by far the highest in the liver, followed by the small intestine, brain, testis and many other organs, but hardly detectable in skeletal muscle and heart. The presence of FAAH in primary cells and cell lines is not universal. FAAH activity is not detectable in human epithelioid carcinoma, HeLa, human larynx epiermoid carcinoma, Hep2, human hepatocellular carcinoma, HepG2, or human astrocytoma cells, CCFSTTG1.The enzyme was found in various cell lines such as mouse neuroblastoma, RBL-2H3, J774, MCF-7, EFM-19 and human neuroblastoma CHP199. Its distribution in organs and tissues, and the inhibitors that have been developed for FAAH that may have therapeutic potential.
References
1.Deutsch DG, et al. Prostaglandins Leukot Essent Fatty Acids. 2002;66(2-3):201–210.
References
1.Deutsch DG, et al. Prostaglandins Leukot Essent Fatty Acids. 2002;66(2-3):201–210.
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)
FAAH
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VU534
产品货号 : M36972
cas no: 923509-20-0
VU534 是一种 NAPE-PLD 激动剂,EC50 为 0.30 μM。VU534 是 FAAH和 sEH (IC50 值为 1.2 μM) 的双重抑制剂。VU534NAPE-PLD 依赖性地增强巨噬细胞的胞葬作用。VU534 具有用于心脏代谢疾病研究的潜力。 -
2-Chlorophenylboronic acid
产品货号 : M36927
cas no: 3900-89-8
2-Chlorophenylboronic acid is a monohalogenated phenylboronic acid, which is an important pharmaceutical intermediate and is widely used in the synthesis of new drugs.2-Chlorophenylboronic acid has an inhibitory effect on fatty acid amidase with a Ki value of 0.01-1 μM, and is used in the study of depression, glaucoma, neuropathic pain, anxiety, migraine, I diabetes and gastritis. , migraine, type I diabetes and gastritis. -
AM 374
产品货号 : M36258
cas no: 86855-26-7
AM 374 是一种脂肪酸酰胺水解酶 (FAAH) 抑制剂。AM 374 对氨基酶活性的抑制作用的 IC50 为 13 nM。AM 374 可用于神经系统疾病的研究。 -
CB2R/FAAH?modulator-1
产品货号 : M36058
cas no: 928892-60-8
CB2R/FAAH modulator-1 是一种大麻素 2 型受体 (CB2R) 完全激动剂,对 CB2R 和 CB1R 的 Ki 分别为 14.8 nM 和 241.3 nM。CB2R/FAAH modulator-1 是一种脂肪酸酰胺水解酶 (FAAH) 抑制剂,IC50 为 4 μM。CB2R/FAAH modulator-1 减少促炎并增加抗炎细胞因子的产生。 -
Dual FAAH/sEH-IN-1
产品货号 : M35726
cas no: 2756099-59-7
Dual FAAH/sEH-IN-1 (compound 3) 是一种高亲和力的双 sEH (可溶性环氧水解酶)和 FAAH (脂肪酸酰胺水解酶)抑制剂,其 IC50 值分别为 9.6 和 7 nM。Dual FAAH/sEH-IN-1 表现出抗炎作用。