FAAH-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/FAAH.html FAAHFatty acid amide hydrolaseFAAH (Fatty acid amide hydrolase) is a membrane-bound protein belonging to serine hydrolase family of enzymes.FAAH isresponsible for the hydrolysis of a number of important endogenous fatty acid amides, including the endo

2、genous cannabimimeticagent anandamide (AEA), the sleep-inducing compound oleamide, and the putative anti-inflammatory agentpalmitoylethanolamide (PEA). FAAH plays a significant role in termination of signalling of a class of bioactive lipids called fatty acidamides (FAAs) both in the central nervous

3、 system (CNS) and peripheral tissues.FAAH belongs to the amidase signature (AS) superfamily and is widely distributed in multicellular eukaryotes. FAAH has a key rolein the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues2-arachidono

4、ylglycerol.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/FAAH.html FAAH HYPERLINK https:/www.MedChemE/Targets/FAAH.html HYPERLINK https:/www.MedChemE/Targets/FAAH.html Inhibitors HYPERLINK https:/www.MedChemE/1-monomyristin.html 1-Monomyristin HYPERLINK https:/www.MedChemE/1-monomyristin.html

5、 HYPERLINK https:/www.MedChemE/aa38-3.html AA38-3Cat. No.: HY-N2512 Cat. No.: HY-185441-Monomyristin, extracted from Serenoa repens,inhibits the hydrolysis of 2-oleoylglycerol(IC =32 M) and fatty acid amide hydrolase (FAAH)50activity (IC =18 M).50AA38-3 is a serine hydrolase (SH) inhibitor.AA38-3 ca

6、n inhibit three SHs, ABHD6, ABHD11, andFAAH.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 99.63%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Acetylhydrolase-IN-1.html Acetylhydrolase-IN-1 HYPERLINK ht

7、tps:/www.MedChemE/Acetylhydrolase-IN-1.html HYPERLINK https:/www.MedChemE/BIA-10-2474.html BIA HYPERLINK https:/www.MedChemE/BIA-10-2474.html HYPERLINK https:/www.MedChemE/BIA-10-2474.html 10-2474Cat. No.: HY-102054 Cat. No.: HY-19740Acetylhydrolase-IN-1 is a1-Alkyl-2-acetylglycerophosphocholine est

8、erase(Alkylacetyl-GPC: acetylhydrolase) inhibtor.BIA 10-2474 is an inhibitor of fatty acid amidehydrolase (FAAH) with IC values of 50 to5070mg/kg in various rat brain regions.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.41%Clinical Data: No Development ReportedSize: 5

9、mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bia-10-2474-d3.html BIA HYPERLINK https:/www.MedChemE/bia-10-2474-d3.html HYPERLINK https:/www.MedChemE/bia-10-2474-d3.html 10-2474-d3Cat. No.: HY-19740S HYPERLINK https:/www.MedChemE/Biochanin-A.html Biochanin HYPERLINK https:/www.MedChemE/Bioc

10、hanin-A.html HYPERLINK https:/www.MedChemE/Biochanin-A.html A(4-Methylgenistein; Olmelin) Cat. No.: HY-14595BIA 10-2474-d3 is the deuterium labeled BIA10-2474. BIA 10-2474 is an inhibitor of fatty acidamide hydrolase (FAAH) with IC values of 50 to5070mg/kg in various rat brain regions.Biochanin A is

11、 a naturally occurring fatty acidamide hydrolase (FAAH) inhibitor, which inhibitsFAAH with IC s of 1.8, 1.4 and 2.4 M for mouse,50rat, and human FAAH, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2

12、00 mg, 500 mg HYPERLINK https:/www.MedChemE/Carprofen.html Carprofen HYPERLINK https:/www.MedChemE/Carprofen.html HYPERLINK https:/www.MedChemE/carprofen-d3.html Carprofen-d3Cat. No.: HY-B1227 Cat. No.: HY-B1227SCarprofen is a nonsteroid anti-inflammatory agent,acts as a multi-target FAAH/COX inhibi

13、tor, withIC s of 3.9 M, 22.3 M and 78.6 M for COX-2,50COX-1 and FAAH, respectively.Carprofen-d3 is the deuterium labeled Carprofen.Carprofen is a nonsteroid anti-inflammatory agent,acts as a multi-target FAAH/COX inhibitor, withIC s of 3.9 M, 22.3 M and 78.6 M for COX-2,50COX-1 and FAAH, respectivel

14、y.Purity: 99.96%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/dual-faah-seh-in-1.html Dual HYPERLINK https:/www.MedChemE/dual-faah-seh-in-1.html HYPERLINK https:/www.MedChemE/dual-faah-seh-in-1.html FAA

15、H/sEH-IN-1 HYPERLINK https:/www.MedChemE/dual-faah-seh-in-1.html HYPERLINK https:/www.MedChemE/faah-inhibitor-1.html FAAH HYPERLINK https:/www.MedChemE/faah-inhibitor-1.html HYPERLINK https:/www.MedChemE/faah-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/faah-inhibitor-1.html HYPERLINK ht

16、tps:/www.MedChemE/faah-inhibitor-1.html 1Cat. No.: HY-144738(Benzothiazole analog 3) Cat. No.: HY-10862Dual FAAH/sEH-IN-1 (compound 3) is a high affinitydual sEH (soluble epoxide hydrolase) and FAAH(fatty acid amide hydrolase) inhibitor, with IC50values of 9.6 and 7 nM, respectively. DualFAAH/sEH-IN

17、-1 shows antinociception against theinflammatory phase.FAAH inhibitor 1 (Benzothiazole analog 3) is apotent fatty acid amide hydrolase (FAAH)inhibitor with an IC of 188 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg,

18、5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/FAAH-IN-1.html FAAH-IN-1Cat. No.: HY-111389 HYPERLINK https:/www.MedChemE/FAAH-IN-2.html FAAH-IN-2(O-Desmorpholinopropyl Gefitinib) Cat. No.: HY-79511FAAH-IN-1 is a fatty acid amide hydrolase (FAAH)inhibitor

19、, with IC s of 145 nM and 650 nM for rat50and human FAAH, respectively.FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is apotent FAAH(fatty acid amide hydrolase) inhibitorextracted from Patent WO/2008/100977A2.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.17%Clinical Data:

20、 No Development ReportedSize: 10 mM 1 mL, 500 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/faah-in-5.html FAAH-IN-5 HYPERLINK https:/www.MedChemE/faah-in-5.html HYPERLINK https:/www.MedChemE/faah-magl-in-1.html FAAH/MAGL-IN-1Cat. No.: HY-146341 Cat. No.: HY-143263FAAH-IN-5 (Compound 7) is a relative s

21、elective,irreversible fatty acid amide hydrolase (FAAH)inhibitor with an IC of 10.5 nM. FAAH-IN-5 shows50low PAMPA (Parallel Artificial MembranePermeability Assay) permeability.FAAH/MAGL-IN-1 (compound SIH 3) is a potent FAAHand MAGL inhibitor with IC s of 31 nM and 2950nM, respectively. FAAH/MAGL-I

22、N-1 has the potentialfor the research of neuropathic pain.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/faah-magl-in-2.html FAAH/MAGL-IN-2 HYPERLINK https:/www.MedChemE/faah-magl-in-2.h

23、tml HYPERLINK https:/www.MedChemE/faah-magl-in-3.html FAAH/MAGL-IN-3Cat. No.: HY-143264 Cat. No.: HY-146342FAAH/MAGL-IN-2 is a potent, reversible, orallyactive, and cross the blood-brain barrier FAAHand MAGL inhibitor with IC s of 11 nM and 3650nM (Ks of 28 nM and 60 nM), respectively .iFAAH/MAGL-IN

24、-3 (Compound 10) is an irreversiblefatty acid amide hydrolase (FAAH) andmonoacylglycerol lipase (MAGL) dual inhibitor withIC values of 179 and 759 nM against FAAH and50MAGL, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Reporte

25、dSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/jnj-1661010.html JNJ-1661010 HYPERLINK https:/www.MedChemE/jnj-1661010.html HYPERLINK https:/www.MedChemE/JNJ-42165279.html JNJ-42165279(Takeda-25) Cat. No.: HY-N7062Cat. No.: HY-19636JNJ-1661010 (Takeda-25) a potent and selectivefatty acid amide hydro

26、lase (FAAH) inhibitor withIC s of 34 and 33 nM for rat FAAH and human FAAH,50respectively. JNJ-1661010 can cross theblood-brain barrier and used as broad-spectrumanalgesics.JNJ-42165279 is a FAAH inhibitor with IC50 of 70 8 nM and 313 28 nM for hFAAH and rFAAH,respectively.Purity: 98.99%Clinical Dat

27、a: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.87%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/JZL195.html JZL195 HYPERLINK https:/www.MedChemE/JZL195.html HYPERLINK https:/www.MedChemE/LY2183240.html LY2183240Cat.

28、No.: HY-15250 Cat. No.: HY-10865JZL195 is a selective and efficacious dual fattyacid amide hydrolase (FAAH) andmonoacylglycerol lipase (MAGL) inhibitorwith IC s of 2 and 4 nM, respectively.50LY2183240 is a highly potent blocker ofanandamide uptake (IC = 270 pM; =540 nM).50 KiLY2183240 is a potent, c

29、ovalent inhibitor of theendocannabinoid-degrading enzyme fatty acid amidehydrolase (FAAH) with an IC of 12.4 nM.50Purity: 99.81%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.07%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgwww.MedChemE

30、3 HYPERLINK https:/www.MedChemE/magl-in-5.html MAGL-IN-5 HYPERLINK https:/www.MedChemE/magl-in-5.html HYPERLINK https:/www.MedChemE/mk-4409.html MK-4409Cat. No.: HY-119283 Cat. No.: HY-12909MAGL-IN-5 is a non-selective lipase inhibitor withIC values of 144, 90, and 14 nM for human50recombinant monoa

31、cylglycerollipase(MAGL),hormone sensitive lipase(HSL), andfatty acid amide hydrolase(FAAH) respectively.MK-4409 is a potent oxazole FAAH inhibitor andcan be used for the research of inflammatory andneuropathic pain.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical

32、Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/n-3-methoxybenzyl-palmitamide.html N-(3-Methoxybenzyl)Palmitamide HYPERLINK https:/www.MedChemE/n-3-methoxybenzyl-palmitamide.html HYPERLINK https:/www.MedChemE/n-benzyloleamide.html N-BenzyloleamideCat. No.: HY-N2428 Cat. N

33、o.: HY-N6923N-(3-Methoxybenzyl)Palmitamide is a promisinginhibitor of FAAH for the treatment of pain,inflammation and CNS degenerative disorders.N-Benzyloleamide is a maccamide isolated fromLepidium meyenii (Maca). N-Benzyloleamideirreversibly inhibits fatty acid amide hydrolase(FAAH). N-benzyloleam

34、ide influences the energymetabolism and reveals antioxidant and antifatigueactivities.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98.29%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/N-Benzylpalmitamide.html N-Benzylpalmitam

35、ide(N-Benzylhexadecanamide; Macamide 1) Cat. No.: HY-N2365 HYPERLINK https:/www.MedChemE/n-benzyllinolenamide.html N-BenzyllinolenamideCat. No.: HY-N3033N-Benzylpalmitamide is a macamide isolated fromLepidium meyenii, acts as an inhibitor offatty acid amide hydrolase (FAAH).N-Benzyllinolenamide is a

36、 natural macamideisolated from Lepidium meyenii, acts as aninhibitor of fatty acid amide hydrolase (FAAH)with an IC of 41.8 M.50Purity: 98.39%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/PF_750

37、.html PF HYPERLINK https:/www.MedChemE/PF_750.html HYPERLINK https:/www.MedChemE/PF_750.html 750 HYPERLINK https:/www.MedChemE/PF_750.html HYPERLINK https:/www.MedChemE/PF-04457845.html PF-04457845Cat. No.: HY-18081 Cat. No.: HY-14376PF 750 is a selective and covalent fatty acidamide hydrolase (FAAH

38、) inhibitor, with IC s50varied from 16.2-595 nM in differentpre-incubation times. Covalently modifies theenzymes active site serine nucleophile.PF-04457845 is a highly efficacious and selectiveFAAH inhibitor with IC values is 7.20.63 nM50and 7.40.62 nM for hFAAH and rFAAH,respectively.Purity: 98.0%C

39、linical Data: No Development ReportedSize: 1 mgPurity: 99.37%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/PF-3845.html PF-3845 HYPERLINK https:/www.MedChemE/PF-3845.html HYPERLINK https:/www.MedChemE/SA_47.html SA HYPERLINK https:/www.MedChe

40、mE/SA_47.html HYPERLINK https:/www.MedChemE/SA_47.html 47Cat. No.: HY-14380 Cat. No.: HY-18080PF-3845 is a potent, selective, irreversible andorally active inhibitor of fatty acid amidehydrolase (FAAH), with a K of 0.23 M. PF-3845iis a covalent inhibitor that carbamylates FAAHsserine nucleophile.SA

41、47 is a selective and potent inhibitor offatty acid amide hydrolase (FAAH) andcarbamate.Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/sa57.html SA57 HYPERLINK https:/www.MedChemE/sa57.html HYPERLINK https:/www.MedChemE/SA72.html SA72Cat. No.: HY-103463 Cat. No.: HY-U00240SA57 is a potent, selective FAAH inhibitor withIC50s