Metabolism

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  1. DHFR inhibitor

    Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis.
  2. Dehydrogenase inhibitor

    Mono-ammonium glycyrrhizinate(AMGZ) is a unique product derived from Licorice root and has an extremely sweet taste.
  3. Protein kinase inhibitor

    Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

  4. Factor Xa inhibitor

    BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

  5. aromatic-L-amino-acid decarboxylase inhibitor

    Carbidopa inhibits aromatic-L-amino-acid decarboxylase, an enzyme important in the biosynthesis of L-tryptophan to serotonin and in the biosynthesis of L-DOPA to Dopamine (DA).
  6. PDE3 inhibitor

    Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP.
  7. EGFR, PKA,PKC inhibitor

    Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.
  8. Carbonic anhydrase inhibitor

    Diclofenamide (or dichlorphenamide) is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class.
  9. PDE inhibitor

    Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
  10. carbonic anhydrase inhibitor

    Dorzolamide HCl is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. Dorzolamide HCl is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.
  11. ACE inhibitor

    Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure.
  12. RAAS inhibitor

    Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril.
  13. 15-PGDH inhibitor

    Glycyrrhetinic acid inhibits the enzymes (15-hydroxyprostaglandin dehydrogenase and delta-13-prostaglandin) that metabolize the prostaglandins PGE-2 and PGF-2α to their respective 15-keto-13,14-dihydro metabolites which are inactive.
  14. xanthine oxidase inhibitor

    Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM).
  15. HMG-CoA reductase inhibitor

    Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
  16. CYP2D6 inhibitor

    Haloperidol (Haldol) is an antipsychotic and butyrophenone.
  17. PDE4 inhibitor

    Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer.
  18. PDE5 inhibitor

    Icariin is inhibitory to all three PDE5 isoforms that inhibits PDE5A1, A2, and A3 with an IC50 value of 1.0, 0.75, and 1.1 microM, respectively.
  19. P450 inhibitor

    As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a constituent of fungal cell membranes, as well as certain enzymes.
  20. Dehydrogenase inhibitor

    Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug) class of drugs. Leflunomide is used to relieve symptoms caused by rheumatoid arthritis, such as inflammation, swelling, stiffness, and joint pain.
  21. PDE4 inhibitor

    Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property.
  22. Hydroxylase Inhibitor

    LX 1606 hippurate is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.
  23. PDE3 inhibitor

    Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE
  24. IMPDH inhibitor

    Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells.
  25. dopamine beta-hydroxylase inhibitor

    Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
  26. DHFR inhibitor

    NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM.
  27. TXAS inhibitor

    Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM.
  28. PDE inhibitor

    Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3).
  29. CYP3A4 inhibitor

    Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
  30. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  31. ACE inhibitor

    Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
  32. HMG-CoA reductase inhibitor

    Rosuvastatin (Crestor) is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins.
  33. mitochondrial electron transport chain complex I inhibitor

    Rotenone is an mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
  34. PDE4 inhibitor

    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  35. MAO Inhibitor

    Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM.
  36. PDE5 inhibitor

    Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
  37. HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  38. HDAC inhibitor

    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.
  39. PDE5 inhibitor

    Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8 nM.
  40. Hydroxylase inhibitor

    Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
  41. Procollagen C-proteinase inhibitor

    UK-383367 is a procollagen C-proteinase inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs.
  42. PDE-5 Inhibitor

    Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.
  43. CYP17 inhibitor

    Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion.
  44. 5-lipoxygenase inhibitor

    Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
  45. CYP17A1 inhibitor

    TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme.
  46. CYP17 inhibitor

    Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1).
  47. PDE Inhibitor

    GSK256066 is an exceptionally high affinity and selective inhibitor of PDE4 that inhibits PDE4 isoforms A-D with equal affinity and has a high HARBS (High-Affinity Rolipram Binding Site) ratio (>17).
  48. CETP inhibitor

    Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.
  49. Monoacylglycerol lipase inhibitor

    URB754 was originally reported to be a potent, noncompetitive inhibitor of monoacylglycerol lipase.
  50. MAO B inhibitor

    Rasagiline is a selective irreversible inhibitor of MAO-B (monoamine oxidase-B).

Items 551-600 of 2992

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