Metabolism

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  1. squalene synthase inhibitor

    RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8??0.2 nM.
  2. 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.

  3. Cytochrome P450 inhibitor

    Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase.
  4. alpha-glucosidase I inhibitor

    Celgosivir is an alpha-glucosidase I inhibitor for the potential treatment of HCV infection.
  5. PDE9 inhibitor

    PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor that increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice.
  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. WNK inhibitor

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

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

  9. dehydroorotate dehydrogenase inhibitor

    Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive drug.
  10. TB5

    hMAO-B inhibitor

    TB5 is a potent, selective and reversible inhibitor of hMAO-B with a Ki value of 0.11??0.01 μM.
  11. 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.
  12. SRPK inhibitor

    SRPIN340 is a cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50 = 0.14 and 1.8 μM, respectively, against mSRPK1 and mSRPK2) with much reduced activity against 143 other kinases.
  13. DGAT-1 inhibitor

    AZD3988 is a diacylglycerol acyl transferase-1 (DGAT-1) inhibitor with IC50s of 6, 5, 11 nM for human, rat, mouse, respectively.
  14. Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor

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

    Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
  16. Cathepsin B inhibitor

    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
  17. PDE5 inhibitor

    Udenafil is a PDE5 inhibitor used in urology to treat erectile dysfunction.
  18. MAO-B inhibitor

    Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration.
  19. SCD1 inhibitor

    A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
  20. SGK1 inhibitor

    GSK 650394 is a glucocorticoid- and serum-regulated kinase 1 (SGK1) inhibitor which displays antiproliferative properties against the LNCaP prostate carcinoma cell line.
  21. PDE3 inhibitor

    Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
  22. NAMPT Inhibitor

    GNE-617 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with IC50 value of 5nM.
  23. LDHA Inhibitor

    AZ33 is a LDHA Inhibitor.
  24. HO-1 inhibitor

    Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.
  25. leukotriene biosynthesis inhibitor

    MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
  26. 15-LO inhibitor

    PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis.
  27. HSP 70 inhibitor

    VER 155008 is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nM).
  28. MAO Inhibitor

    Bifemelane hydrochloride is an antidepressant MAO inhibitor. Reverses catalepsy induced by tetrabenazine in mice and increases locomotor activity in MPTP-treated marmosets.
  29. LSD1/BHC110 & MAO inhibitor

    Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor.
  30. ABT

    Cytochrome P450 inhibitor

    ABT (1-Aminobenzotriazole )is a suicide substrate for (CYP)cytochrome P-450 and chloroperoxidase.
  31. Cytochrome P450 inhibitor

    Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.
  32. YZ9

    PFKFB3 inhibitor

    YZ9 is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase) inhibitor with IC50 value of 0.183 μM.
  33. cathepsin S inhibitor

    Petesicatib is a cathepsin S inhibitor, used in research of immune diseases.
  34. Xanthine oxidase inhibitor

    Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout.
  35. PDE4 inhibitor

    MK-0359 is a selective and potent oral PDE4 inhibitor, in chronic asthma.
  36. Cathepsin S inhibitor

    Z-FL-COCHO (LY3000328) is a novel Cathepsin S inhibitor.

     
  37. hIDO2 inhibitor

    GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.
  38. CYP17A1/androgen synthesis inhibitor

    Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.
  39. HSD1 inhibitor

    AZD4017 is a potent, selective, and orally bioavailable11b-HSD1 inhibitor (11b-hydroxysteroid dehydrogenase type 1 inhibitor).
  40. Cathepsin B inhibitor

    CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.
  41. Carbonic anhydrase inhibitor

    Benzenesulfonamide ia an inhibitor of carbonic anhydrases.
  42. PDE3 inhibitor

    Cilostamide is a selective inhibitor of phosphodiesterase (PDE)3A and PDE3B with IC50 values of 27 and 50 nM, respectively.
  43. PDE9A Inhibitor

    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
  44. HSP90-calcineurin-NFAT inhibitor

    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation.
  45. ACE inhibitor

    Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
  46. HMG-CoA reductase inhibitor

    Mevastatin is an inhibitor of HMG-CoA reductase.
  47. PDE-KRAS inhibitor

    Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
  48. HMG-CoA reductase inhibitor

    Atorvastatin is an HMG-CoA reductase inhibitor (IC50 = 154 nM) that is effective in treating hypercholesterolemia and certain dyslipidemias.
  49. 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.
  50. ATP-citrate lyase inhibitor

    BMS303141 is a potent inhibitor of ATP citrate lyase (ACL). BMS303141 inhibits lipid synthesis in HepG2 cells with an IC50 of 8 μM, and lowers plasma triglycerides in a murine hyperlipdemia model.

Items 201-250 of 756

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