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)
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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(30)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
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Lipoxygenase(0)
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Other Targets(10)
P450(112)
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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
catalog no : M36972
cas no: 923509-20-0
VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.VU534 is a dual inhibitor of FAAH and sEH, with an IC50 of 1.2 μM for sEH.VU534 is used in diseases related to cardiometabolism. -
2-Chlorophenylboronic acid
catalog no : 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. -
AM 374
catalog no : M36258
cas no: 86855-26-7
AM 374 (HDSF), a fatty acid amide hydrolase (FAAH) inhibitor, demonstrates the capacity to inhibit amidase activity, boasting an IC50 value of 13 nM. -
CB2R/FAAH?modulator-1
catalog no : M36058
cas no: 928892-60-8
CB2R/FAAH?modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. -
Dual FAAH/sEH-IN-1
catalog no : M35726
cas no: 2756099-59-7
Dual FAAH/sEH-IN-1 is a dual inhibitor of sEH (soluble epoxide hydrolase) (IC50: 9.6 nM) and FAAH (fatty acid amide hydrolase) (IC50: 7 nM) with high affinity and anti-inflammatory activity.