Lipase

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  1. Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL.
  2. Tanshinone IIA (TIIA) is one of the major extracts obtained from Salvia miltiorrhiza BUNGE, which has anti-inflammatory and anti-apoptotic effects on many diseases.
  3. Monoacylglycerol lipase inhibitor

    URB754 was originally reported to be a potent, noncompetitive inhibitor of monoacylglycerol lipase.
  4. dual FAAH/MAGL inhibitor

    JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL respectively.
  5. MAGL Inhibitor

    JZL184 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nM).
  6. Endothelial lipase(EL) inhibitor

    XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
  7. hormone sensitive lipase (HSL) inhibitor

    HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC50=2 nM) with a significantly reduced reactive metabolite liability.
  8. MAGL inhibitor

    JW-642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
  9. ATGL inhibitor

    Atglistatin is a highly potent, selective and competitive inhibitor of adipose triglyceride lipase (ATGL) with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, but no toxicity up to a concentration of 50 μM.
  10. Dihydroberberine is an inhibitor of pancreatic lipase with IC50 value of 8 mg/ml.
  11. lipase inhibitor

    Cetilistat is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine.
  12. MAGL inhibitor

    MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA).
  13. MGL inhibitor

    URB602 is a selective inhibitor of monoglycerol lipase (MGL), exhibiting an IC50 of 28 μM for the rat brain enzyme.
  14. diacylglycerol lipase (DAGL) inhibitor

    DO34 is a novel potent and selective diacylglycerol lipase (DAGL) inhibitor.
  15. MAGL inhibitor

    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  16. ABHD6 inhibitor

    KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
  17. ABHD6 inhibitor

    KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
  18. ABHD12 inhibitor

    DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
  19. ABHD6 inhibitor

    KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
  20. covalent MAGL inhibitor

    PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM.
  21. MAGL inhibitor

    JJKK 048 is an ultrapotent and highly selective inhibitor of Monoacylglycerol lipase (MAGL).
  22. endothelial lipase inhibitor

    Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.
  23. ABHD6 inhibitor

    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
  24. MAGL inhibitor

    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.

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