Metabolism

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  1. PDE-2 Inhibitor

    BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human).
  2. Collagen proline hydroxylase inhibitor

    Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor.
  3. factor Xa inhibitor

    Otamixaban(FXV 673) is an intravenous direct factor Xa inhibitor.
  4. PDE-9 inhibitor

    PDE-9 inhibitor is useful for neurodegenerative diseases.
  5. MAO-B Inhibitor

    SL-251188, an oxazolidinone derivative, was characterized in baboons as a radioligand for the in vivo visualization of MAO-B using positron emission tomography (PET).
  6. 2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells.
  7. PDE3 inhibitor

    SDZ-MKS 492 (MKS 492) is a selective type III isozyme inhibitor of cyclic nucleotide phosphodiesterase, effective in allergic bronchoconstriction and platelet activating factor (PAF) or LTB4-induced inflammatory reactions in animals.
  8. CYP3A4 enzyme inhibitor

    Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
  9. FOXO relocator

    LOM612 is a potent FOXO relocator, with an EC50 value of 1.5 μM in cells.
  10. DGAT1 inhibitor

    Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor.
  11. PPAR-α/γ agonist

    Aleglitazar is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.
  12. Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca2+ influx, and DHT-like effects.
  13. IDH1 R132H inhibitor

    IDH-C227 is a potent and selective IDH1 R132H inhibitor.
  14. NAMPT activator

    (R)-P7C3-Ome is a methoxy derivative of parent compound P7C3, an aminopropyl carbazole that exhibits antidepressant and neuroprotective activities.
  15. PDE9A inhibitor

    BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM.
  16. FASN inhibitor

    Denifanstat (TVB-2640) is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM.

  17. WNK inhibitor

    WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
  18. GA mitochondrial matrix inhibitor

    Gamitrinib TPP is a GA mitochondrial matrix inhibitor. Gamitrinib TPP is offered as the hexafluorophosphate salt.

  19. N2-methylguanosine is a modified nucleoside that occurs at several specific locations in many tRNA's.
  20. Megakaryocytes/platelets inducing agent is an inducing agent for megakaryocytes and/or platelets from pluripotent stem cells, the inducing agent being useful in treating diseases involving thrombopenia.
  21. Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor

    Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM.
  22. LDHA Inhibitor

    AZ33 is a LDHA Inhibitor.
  23. Isotetrandrine is a biscoclaurine alkaloid inhibitor of G protein activation of PLA2 but not PLC or PLD.
  24. factor Xa inhibitor

    DPC423 is a highly potent and orally bioavailable pyrazole antithrombotic agent.
  25. Afegostat D-tartrate was an experimental drug for the treatment of certain forms of Gaucher's disease. The substance was used in form of the tartrate. Isofagomine (IFG) is an acid β-glucosidase (GCase) active site inhibitor that acts as a pharmacological chaperone.
  26. Licochalcone C was synthesized from commercially available 2,4-dihydroxybenzaldehde by using regioselective Al2O3-mediated C-prenylation followed by conventional Claisen-Schmidt condensation in basic condition.
  27. DGAT-1 inhibitor

    ABT-046 is a potent, selective, and orally bioavailable Diacylglycerol acyltransferase 1 (DGAT-1 ) inhibitor (IC50= 8 nM).
  28. FLAP inhibitor

    AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively.
  29. DGAT1 inhibitor

    AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1).
  30. SGK inhibitor

    EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 uM.
  31. PDE Inhibitor

    GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.
  32. Impurity of Calcipotriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  33. PPARγ agonist

    Inolitazone dihydrochloride is a novel high-affinity PPARγ agonist, which activates PPARγ with an EC50 about 1/50 that of rosiglitazone and has no effect on RIE cells.
  34. HSP90 inhibitor

    Macbecin I is an ansamycin antibiotic compound that inhibits Hsp90 activity with IC50 value of μM by binding to the ATP-binding site.
  35. FXR agonist

    LY2562175 is a potent and selective FXR agonist in vitro and has robust lipid modulating properties, lowering LDL and triglycerides while raising HDL in preclinical species.
  36. TRPM8 Antagonist

    AMG-333 is a potent and selective TRPM8 Antagonist.
  37. PUN30119, also known as Imidazole ketone erastin (IKE), is a potent, metabolically stable inhibitor of system xc- and inducer of ferroptosis potentially suitable for in vivo applications.
  38. Fer and FerT inhibitor

    E260 is a novel inhibitor of the Fer/FerT kinase with Kd of 0.85 uM.
  39. penicillin binding protein inhibitor

    Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.
  40. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses.
  41. PDE4D inhibitor

    BPN14770 is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
  42. L-Palmitoylcarnitine is a fatty acid metabolite.
  43. 5-LOX inhibitor

    PF-4191834 is a novel, potent and selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain with an IC50=229 nM. displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes.
  44. IDH1 inhibitor

    Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia.
  45. Stearoylethanolamide is an endocannabinoid-like compound with pro-apoptotic activity.
  46. Hydroxypyruvic acid is an intermediate in the metabolism of Glycine, serine and threonine. It is a substrate for Serine--pyruvate aminotransferase and Glyoxylate reductase/hydroxypyruvate reductase.
  47. IDO inhibitor

    IDO-IN-12 is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO 2017181849 A1.
  48. Stigmastanol is a phytosterol found in a variety of plant sources.
  49. Glutarylcarnitine is the diagnostic metabolite for malonic aciduria and glutaric aciduria type I monitored in most tandem mass spectrometry newborn screening programmes.

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