Metabolism

Items 101-150 of 1392

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Product Name
Application
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Product Citation
  1. ACE inhibitor

    Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
  2. Ranolazine is a partial fatty acid oxidation inhibitor, shifts ATP production from fatty acid to more oxygen-efficient carbohydrate oxidation.
  3. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP).
  4. Factor Xa inhibitor

    Rivaroxaban is an oxazolidinone derivative optimized for inhibiting both free Factor Xa and Factor Xa bound in the prothrombinase complex.
  5. PDE inhibitor

    Roflumilast acts as a selective, long-acting inhibitor of the enzyme PDE-4.
  6. PDE4 inhibitor

    Rolipram is a PDE4-inhibitor with IC50 = 2.0 μM.
  7. PPAR agonist

    Rosiglitazone works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
  8. PPAR agonist

    Rosiglitazone maleate, an antidiabetic drug, works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
  9. 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.
  10. 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.
  11. 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.
  12. MAO Inhibitor

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

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

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  15. Sodium danshensu is a sodium salt of danshensu from the widely used Chinese herb Danshen (Salvia miltiorrhiza Bunge). In vitro and in vivo studies revealed that danshensu possessed diverse pharmacological effects, including relaxation of coronary artery, anticoagulation, protection of myocardial ischemia-reperfusion injury, and antiarrhythmia activities
  16. 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.
  17. Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
  18. PDE5 inhibitor

    Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8 nM.
  19. Phospholipase inhibitor

    Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.
  20. 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.
  21. Tazarotene is a prodrug and a member of the acetylenic class of retinoids.
  22. Hydroxylase inhibitor

    Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
  23. FTase inhibitor

    Tipifarnib (Zarnestra) is a farnesyltransferase inhibitor that inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive.
  24. RAR agonist

    Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors).
  25. Trilostane is an inhibitor of 3??-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
  26. Procollagen C-proteinase inhibitor

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

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

    Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion.
  29. 5-lipoxygenase inhibitor

    Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
  30. PDE Inhibitor

    Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells.
  31. Hsp90 inhibitor

    Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.
  32. CYP17A1 inhibitor

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

    URB597 is a relatively selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH).
  34. 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).
  35. HSP90 Inhibitor

    AT13387 is a targeted inhibitor of Hsp90,inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival.
  36. 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).
  37. Hsp90 inhibitor

    PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.
  38. CETP inhibitor

    Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.
  39. Retinoid X Receptor Ligand

    Bexarotene is a highly selective retinoid X receptor (RXR) agonist.
  40. Monoacylglycerol lipase inhibitor

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

    Rasagiline is a selective irreversible inhibitor of MAO-B (monoamine oxidase-B).
  42. HMG-CoA reductase inhibitor

    Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease.
  43. Hsp90 Inhibitor

    PU-H71 is a potent Hsp90 inhibitor (IC50 = 50 nM).
  44. Hsp90 inhibitor

    MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
  45. Peroxisome Proliferator

    Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology.
  46. CYP17 inhibitor

    TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.
  47. FXR agonist

    GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).
  48. TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.
  49. DBH inhibitor

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

  50. FAAH Inhibitor

    PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It reduces inflammatory pain via a cannabinoid receptor-dependent mechanism.

Items 101-150 of 1392

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