Metabolism

Items 2001-2050 of 6503

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  1. DHFR inhibitor

    Pemetrexed is a novel antifolate with multiple targets
  2. PPARα/γ dual agonist

    Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
  3. PDE-4-D inhibitor

    CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
  4. Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca2+ influx, and DHT-like effects.
  5. HSF1 activation inhibitor

    Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
  6. PDE4 inhibitor?€?

    AN2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines
  7. Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.
  8. glucokinase activator

    GKA50 is a potent activator of glucokinase
  9. Cerpegin is a naturally occurring pyridinone alkaloid isolated from Roxb, a tradional indian medicine used as an anti-inflammatory, analgesic, antiulcer and tranquilizer.
  10. factor Xa inhibitor

    Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa.
  11. factor Xa inhibitor

    Letaxaban, also known as TAK-442, is a potent, selective, and orally active factor Xa inhibitor, which is a tetrahydropyrimidin-2(1H)-one derivative. TAK-442 inhibited endogenous FXa activity in platelet-poor human [half-maximal inhibitory concentration (IC(50)): 53 nM, TAK-442] and rat (IC(50): 32 nM, TAK-442) plasma.
  12. COX/5-LOX inhibitor

    Tepoxalin is a dual cyclooxygenase/5-lipoxygenase inhibitor of arachidonic acid metabolism with potent anti-inflammatory activity and a favorable gastrointestinal profile
  13. SCD1 inhibitor

    stearoyl-CoA desaturase 1 (SCD1) inhibitor. Used to selectively eliminate undifferentiated human pluripotent stem cells (hPSCs) from culture; induces ER stress, attenuates protein synthesis and induces apoptosis in hPSCs. Prevents teratoma formation in immunocompromised mice.
  14. IDH1 inhibitor

    AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity.
  15. IDH2 R140Q inhibitor

    AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.
  16. AR7

    RARα antagonist.

    AR7 was developed as a highly potent and selective enhancer of the chaperone-mediated autophagy (CMA) through antagonizing RARα.
  17. PDE inhibitor

    Forskolin is a cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties.
  18. IDH1 R132H inhibitor

    IDH-C227 is a potent and selective IDH1 R132H inhibitor.
  19. NAMPT activator

    P7C3 is neurogenic and protects new neurons against apoptosis. It protects newborn neurons in the dentate gyrus and stimulates the growth of new neurons.
  20. NAMPT activator

    (R)-P7C3-Ome is a methoxy derivative of parent compound P7C3, an aminopropyl carbazole that exhibits antidepressant and neuroprotective activities.
  21. Homogentisic acid is a specific metabolite in urine and serum, which is used for diagnosis of alkaptonuria.
  22. AhR antagonist

    StemRegenin 1 (SR1) is a cell-permeable purine derivative that acts as an antagonist of aryl hydrocarbon receptor and promotes the self-renewal of hematopoietic stem cells (HSCs).
  23. MAO-A inhibitor

    Salsolidine is a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A inhibitor.
  24. PDE9A inhibitor

    BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM.
  25. CRM1 Inhibitor

    KPT185 is a selective CRM1 inhibitor. KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts.
  26. HIF inhibitor

    BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I.
  27. IDO1 inhibitor

    INCB024360 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities.
  28. PDE2A inhibitor

    PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.
  29. RAR agonist

    TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs).
  30. oxidative phosphorylation inhibitor

    Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma. Gboxin inhibits the activity of F0F1 ATP synthase. Antitumour activity.
  31. squalene synthase inhibitor

    RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8??0.2 nM.
  32. FASN inhibitor

    Denifanstat (TVB-2640) is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM.

  33. Cytochrome P450 inhibitor

    Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase.
  34. alpha-glucosidase I inhibitor

    Celgosivir is an alpha-glucosidase I inhibitor for the potential treatment of HCV infection.
  35. PDE9 inhibitor

    PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor that increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice.
  36. L-Valyl-L-phenylalanine (Valylphenylalanine; H-VAL-PHE-OH) has been reported as biocompatible polymer.
  37. peripheral benzodiazepine receptor agonist

    AC-5216 is a translocator protein [TSPO (18 kDa)] ligand.
  38. Endothelial lipase(EL) inhibitor

    XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
  39. WNK inhibitor

    WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
  40. glucokinase activator

    PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 ?μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus.
  41. Benzo[a]pyrene shows lung carcinogenicity in animal models, and it is frequently used in chemoprevention studies.
  42. GA mitochondrial matrix inhibitor

    Gamitrinib TPP is a GA mitochondrial matrix inhibitor. Gamitrinib TPP is offered as the hexafluorophosphate salt.

  43. dehydroorotate dehydrogenase inhibitor

    Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive drug.
  44. TB5

    hMAO-B inhibitor

    TB5 is a potent, selective and reversible inhibitor of hMAO-B with a Ki value of 0.11??0.01 μM.
  45. hormone sensitive lipase (HSL) inhibitor

    HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC50=2 nM) with a significantly reduced reactive metabolite liability.
  46. N2-methylguanosine is a modified nucleoside that occurs at several specific locations in many tRNA's.
  47. SRPK inhibitor

    SRPIN340 is a cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50 = 0.14 and 1.8 μM, respectively, against mSRPK1 and mSRPK2) with much reduced activity against 143 other kinases.
  48. endogenous trace amine neuromodulor

    m-Tyramine is an endogenous trace amine neuromodulor. m-Tyramine has effects on the adrenergic and dopaminergic receptor.
  49. DGAT-1 inhibitor

    AZD3988 is a diacylglycerol acyl transferase-1 (DGAT-1) inhibitor with IC50s of 6, 5, 11 nM for human, rat, mouse, respectively.
  50. Megakaryocytes/platelets inducing agent is an inducing agent for megakaryocytes and/or platelets from pluripotent stem cells, the inducing agent being useful in treating diseases involving thrombopenia.

Items 2001-2050 of 6503

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