Metabolism

Items 2101-2150 of 6503

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  1. Autotaxin inhibitor

    PF-8380 is a potent and specific autotaxin inhibitor with an IC50 value of 2.8 nM.
  2. PDE-9 inhibitor

    PDE-9 inhibitor is useful for neurodegenerative diseases.
  3. Paricalcitol is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.
  4. PC-PLC inhibitor

    SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.
  5. SMND-309 is a metabolite of salvianolic acid B, and exhibits neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats.
  6. PPAR-γ antagonist

    T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2.
  7. RARα agonist

    Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.
  8. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  9. anticancer and radioprotection agent

    Geniposidic acid is an effective anticancer and radioprotection agent.
  10. antitumor agent

    Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
  11. Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.
  12. Carbonic anhydrase inhibitor

    Tioxolone is an anti-acne preparation.
  13. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body.
  14. PPARγ agonist

    Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α.
  15. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination.
  16. Monoamine oxidase inhibitor

    Rasagiline is an irreversible inhibitor of monoamine oxidase used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases. It is selective for MAO type B over type A by a factor of fourteen.
  17. Edaravone is a free radical scavenger with diverse protective effects that inhibits production of reactive oxygen species, apoptosis and the lipoxygenase system.
  18. Ciprofibrate is a peroxisome proliferator-activated receptor agonist.
  19. Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I.
  20. Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme inhibitor (ACE) which is used for the treatment of hypertension and congestive heart failure.
  21. ACE inhibitor

    Cilazapril is a pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure.
  22. ACE inhibitor

    Fosinopril is an angiotensin converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of chronic heart failure.
  23. ACE inhibitor

    Temocapril is an ACE inhibitor.
  24. Probucol lowers the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism. Additionally, probucol may inhibit cholesterol synthesis and delay cholesterol absorption.
  25. Carbonic anhydrase inhibitor

    Brinzolamide is a carbonic anhydrase inhibitor.
  26. 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).
  27. Serotonin synthesis inhibitor

    LX 1606 is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.
  28. RARα agonist

    AM 580 is an analog of retinoic acid that acts as a selective RARα agonist.
  29. RARγ-selective agonist

    CD 437 is a synthetic retinoid that is an RARγ-selective agonist.
  30. HMG-CoA reductase inhibitor

    Atorvastatin (Lipitor) is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol.
  31. anti-inflammatory corticosteroid

    Clobetasol propionate is a anti-inflammatory corticosteroid used to treat various skin disorders.
  32. Imidapril (Tanatril) is an inhibitor of angiotensin converting enzyme (ACE).
  33. Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes.
  34. HMG-CoA reductase inhibitor

    Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM, used for lowering cholesterol (hypolipidemic agent).
  35. HMG-CoA reductase inhibitor

    Pravastatin sodium is a water-soluble, competitive inhibitor of 3-hydroxy-3-methyl coenzyme A (HMG-CoA) reductase. Potently blocks cholesterol synthesis in vivo (Ki~ 1 nM) and displays cardioprotective properties.
  36. FAAH inhibitor

    LY 2183240 acts both as a potent inhibitor of the reuptake of the endocannabinoid anandamide, and as an inhibitor of fatty acid amide hydrolase (FAAH), the primary enzyme responsible for degrading anandamide.
  37. TMS
    TMS is a potent, selective and competitive inhibitor of cytochrome P450 1B1, an enzyme overexpressed in certain tumors (IC50= 6 nM). 5N/A- and 520-fold selective over P450 1A1 and 1A2 respectively.
  38. PPARα agonist

    GW 7647 is a potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively).
  39. PPARδ agonist

    L-165,041 is a potent PPARδ agonist (Ki = 6 nM); displays > 100-fold selectivity for both mouse and human PPARδ receptors over other subtypes.

  40. PPARγ antagonist

    GW 9662 is a selective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively).
  41. IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
  42. Cathepsin K inhibitor

    Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys.
  43. Uracil-d4 is the labelled compound form of Uracil which is a nitrogenous base on RNA nucleosides.
  44. Ginkgetin, a Biflavone from Ginko biloba leaves, inhibits cyclooxygenases-2 and 5-lipoxygenase in mouse bone marrow-derived mast cells.
  45. Carbonic anhydrase inhibitor

    Punicalin is a highly active carbonic anhydrase inhibitor.
  46. HMG-CoA reductase inhibitor

    Swertiamarin has shown potential as antiatherogenic agent by inhibiting HMG-CoA reductase activity in high cholesterol fed rats.
  47. Vitexin demonstrates antioxidant activity in a DPPH bleaching assay (IC50 = 24.2uM) and also inhibits the activity of the carbohydrate-hydrolyzing enzyme α-glucosidase (IC50 = 244 uM).
  48. thrombin/factor Xa dual inhibitor

    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  49. 5-Amino-3H-imidazole-4-Carboxamide (AICA) is an important precursor for the synthesis of purines in general and of the nucleobases adenine and guanine in particular.
  50. RAR agonist

    Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo.

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