Metabolism

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  1. HSP90 inhibitor

    17-AAG is an ansamycin antibiotic which acts as an anti-tumor agent. Specifically, 17-AAG binds and inhibits Hsp90.
  2. Hsp90 inhibitor

    17-DMAG is a water-soluble analog of 17-AAG and geldanamycin that binds the ATP binding site of Hsp90 and inhibits its chaperone activity. Displays more potent antitumor activity than 17-AAG.
  3. CYP17 inhibitor

    Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1), an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues.
  4. DHFR inhibitor

    Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis.
  5. Anti-Diabetic Agent

    Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes.
  6. Acitretin is a second generation retinoid and is typically used for psoriasis.
  7. Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions.
  8. CYP17 inhibitor

    Alizarin is novelly used as a staining agent in biological research because it stains free calcium and certain calcium compounds a red or light purple color.
  9. Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase.
  10. Adenosine receptor antagonist

    Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.
  11. Dehydrogenase inhibitor

    Mono-ammonium glycyrrhizinate(AMGZ) is a unique product derived from Licorice root and has an extremely sweet taste.
  12. 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.

  13. Factor Xa inhibitor

    Apixaban is an anticoagulant for the prevention of venous thromboembolism and venous thromboembolic events.
  14. CYP17 inhibitor

    Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor.
  15. Lipoxygenase Inhibitor

    Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 µM.

  16. Benserazid hydrochloride is an inhibitor of L-aromatic amino acid decarboxylase.
  17. Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.

  18. HSP90 inhibitor

    BIIB021 is an oral fully synthetic Hsp90 inhibitor that selectively and potently inhibits the molecular chaperone Hsp90 thereby inhibiting the proper assembly of multiple oncogenic proteins involved in tumor growth and survival.
  19. Factor Xa inhibitor

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

  20. Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine (5'-DFCR) and 5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-fluorouracil.

  21. 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).
  22. Carmofur is a pyrimidine analogue used as an antineoplastic agent. It is a derivative of fluorouracil.
  23. Celastrol is a triterpenoid antioxidant compound isolated from the Chinese Thunder of God vine (T. wilfordii). In an isolated rat liver assay of lipid peroxidation, celastrol had an IC50 value of 7 µM, equivalent to about 15 times the antioxidant potency of α-tocopherol.

  24. Chloramphenicol is a bacteriostatic antimicrobial.
  25. Chlorpromazine is a dopamine antagonist of the typical antipsychotic class of medications possessing additional antiadrenergic, antiserotonergic, anticholinergic and antihistaminergic properties used to treat schizophrenia.
  26. PDE-4 inhibitor

    Cilomilast is orally active and acts as a selective Phosphodiesterase-4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with COPD.
  27. PDE3 inhibitor

    Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP.
  28. Cladribine is a synthetic anti-cancer agent that mimics the nucleoside adenosine and thus inhibits the enzyme adenosine deaminase, which interferes with the cell's ability to process DNA.
  29. cytochrome P4503A4 inhibitor

    Clarithromycin is a macrolide antibiotic. It prevents bacteria from growing by interfering with their protein synthesis.
  30. Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL.
  31. Action of clotrimazole is against the division and growing of fungi.Clotrimazole alters the permeability of the fungal cell wall and inhibits the activity of enzymes within the cell. It specifically inhibits the biosynthesis of ergosterol and other sterols required for cell membrane production.
  32. NMDA antagonist

    Non-opioid analgesic with muscle relaxant properties.
  33. 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.
  34. DNA Methyltransferase Inhibitors

    Decitabine is a hypomethylating agent.It hypomethylates DNA by inhibiting DNA methyltransferase.
  35. Iron chelator

    Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.
  36. Carbonic anhydrase inhibitor

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

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