Metabolism

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  1. PDE4 inhibitor

    BW-A78U is a PDE4 inhibitor with an IC50 of 3 μM.
  2. COX and lipo-oxygenase inhibitor

    Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
  3. GAK inhibitor

    SGC GAK 1 is a high affinity cyclin G associated kinase (GAK) inhibitor.
  4. PHGDH inhibitor

    NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with an IC50 value of 2.5 μM.
  5. TLR/SCD inhibitor

    E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).

  6. uPA inhibitor

    UK-371804 is a potent urokinase-type plasminogen activator (uPA) inhibitor.
  7. FAAH inhibitor

    BIA10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) .
  8. RNR Inhibitor

    COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity.
  9. Heparanase inhibitor

    OGT-2115 is a heparanase inhibitor with IC50 value of 0.4 μM.
  10. exportin-1 inhibitor

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  11. PFKFB3 inhibitor

    AZ-PFKFB3-67 is a novel potent and selective PFKFB3 inhibitor.
  12. PUN30119, also known as Imidazole ketone erastin (IKE), is a potent, metabolically stable inhibitor of system xc- and inducer of ferroptosis potentially suitable for in vivo applications.
  13. Fer and FerT inhibitor

    E260 is a novel inhibitor of the Fer/FerT kinase with Kd of 0.85 uM.
  14. alpha-adrenergic receptor agonist / MAO inhibitor

    Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release.
  15. ER stress inhibitor

    Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is an endoplasmic reticulum (ER) stress inhibitor.
  16. CYP2C9 inhibitor

    Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
  17. MAO inhibitor

    Pargyline hydrochloride is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension.
  18. CA9 inhibitor

    Benzthiazide is a long-acting diuretic and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells.
  19. monoamine oxidase A inhibitor

    Clorgyline hydrochloride is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A) that is used in scientific research; structurally related to Pargyline.
  20. Carbonic anhydrase inhibitor

    Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.
  21. Cytochrome P450 inhibitor

    Proadifen hydrochloride is a Cytochrome P450 inhibitor (IC50 = 19μM).
  22. MAO inhibitor

    Iproniazid is a non-selective, irreversible monoamine oxidase (MAO) inhibitor (MAOI) that is used as an antidepressive agent.
  23. PDE4B inhibitor

    Ademetionine, also known as AdoMet; MSI-195; SAMe, S-adenosylmethionine, is a PDE4B inhibitor potentially for treatment of primary biliary cirrhosis and major depressive disorder.
  24. penicillin binding protein inhibitor

    Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.
  25. MAO inhibitor

    Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
  26. MAO-A inhibitor

    Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
  27. CoA reductase inhibitor

    Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor.
  28. Pyruvate dehydrogenase kinase inhibitor

    Sodium Dichloroacetate, also known as CPC-211; DCA; X-11S, is a Pyruvate dehydrogenase kinase inhibitor potentially for the treatment of myocardia ischemia, ischemic. Sodium dichloroacetate also exhibits anti-leukemic activity in B-chronic lymphocytic leukemia (B-CLL) and synergizes with the p53 activator Nutlin-3. Sodium dichloroacetate (DCA) reduces apoptosis in colorectal tumor hypoxia.
  29. monoamine oxidase inhibitor

    Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC50 of 4.8 μM for rat brain monoamine oxidase in vitro.
  30. factor Xa inhibitor

    Fondaparinux sodium is a factor Xa inhibitor to form the high affinity binding site for the anti-coagulant factor antithrombin III (ATIII).
  31. PDE5 inhibitor

    Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  32. MAO-A inhibitor

    Toloxatone (MD 69276) is a reversible monoamine oxidase A (MAOA) inhibitor. Antidepressant.
  33. PDE-5 inhibitor

    Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
  34. MAO inhibitor

    Iproniazid phosphate is an irreversible inhibitor of monoamine oxidase types A and B that is used as an antidepressive agent. It has also been used as an antitubercular agent, but its use is limited by its toxicity.
  35. PDE3 inhibitor

    Fosphenytoin Sodium is the sodium salt form of fosphenytoin, a prodrug that is hydrolyzed to the anticonvulsant phenytoin. It is an PDE3 (phosphodiesterase 3) inhibitor.
  36. PTK inhibitor

    ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
  37. 12-Lipoxygenase (12-LOX) inhibitor

    ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
  38. ATP-competitive STK19 inhibitor

    ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo.
  39. PDE5 inhibitor

    TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6.
  40. MAO inhibitor

    Olodaterol is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim.
  41. FPTase inhibitor

    L-778123 HCl is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.
  42. 15-PGDH enzyme inhibitor

    SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.
  43. PDE10A inhibitor?€?

    TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
  44. ACL inhibitor and AMPK activator

    ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
  45. cytochrome P450 inhibitor

    Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
  46. Carbonic Anhydrase Inhibitor

    Acetazolamide, a potent carbonic anhydrase (CA) inhibitor, is commonly used in clinical practice as an immediate and readily available option for acute reduction of intraocular pressure(IOP).
  47. Dehydrogenase Inhibitor

    AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
  48. Glucose Transporter Inhibitor I

    WZB117 is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 uM.
  49. hALDH1 Inhibitor

    NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
  50. STK33 inhibitor

    ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.

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