Metabolism

Items 151-200 of 6503

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  1. PPARα agonist

    WY 14643 is a highly potent PPARα agonist.
  2. potent cerebroprotection

    Dehydroascorbic acid, a blood-brain barrier transportable form of vitamin C, mediates potent cerebroprotection in experimental stroke.
  3. FTase inhibitor

    FTI 276 is an inhibitor that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific actvation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.
  4. GAPDH inhibitor

    CGP 3466B maleate is an orally active glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor.
  5. 4-Pyridoxic acid is a catabolic product of vitamin B6 which is excreted in the urine.
  6. HSP70 Inhibitor

    Occupies mortalin-2 (mot-2), a member of the Hsp70 family, at its p53 binding site and enables p53 translocation to the nucleus. Selectively cytotoxic; causes growth arrest of cancer cells in culture. Also inhibits telomerase activity and cross-links F-actin.
  7. PPAR antagonist

    GSK-3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6).
  8. PPARδ antagonist

    GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and ??? 10 μM at PPARβ, PPARα and PPARγ respectively).
  9. Rivaroxaban is an oxazolidinone derivative optimized for inhibiting both free Factor Xa and Factor Xa bound in the prothrombinase complex.
  10. FAAH inhibitor

    JNJ 1661010 is a selective and reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12nM).
  11. Palovarotene is a novel retinoic acid receptor gamma agonist for the treatment of emphysema
  12. Dihydroorotate Dehydrogenase Inhibitor

    Brequinar is an inhibitor of dihydroorotate dehydrogenase, an enzyme that is required for de novo pyrimidine biosynthesis.
  13. 5-LPO inhibitor

    ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor.
  14. DGAT1 inhibitor

    Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor.
  15. Cathepsin K inhibitor

    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor.
  16. PPAR-α/γ agonist

    Aleglitazar is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.
  17. squalene synthetase inhibitor

    YM-53601 free base is a squalene synthetase inhibitor which suppresses lipogenic biosynthesis and lipid secretion in rodents.
  18. NAMPT inhibitor

    CHS-828 is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM.
  19. FXa Inhibitor

    Betrixaban is an anticoagulant drug which acts as a direct factor Xa inhibitor. It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low hERG affinity.
  20. CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
  21. CYP3A4 inhibitor

    PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively).
  22. FXR agonist

    Lithocholic acid is a bile acid that acts as a detergent to solubilize fats for absorption.
  23. PDE 3/4 inhibitor

    Zardaverine is a phosphodiesterase inhibitor, selective for PDE3 and 4 (IC50 values are 0.5 and 0.8 uM respectively).
  24. PKR activator

    PKR-IN-2 is a pyruvate kinase (PKR) activator.
  25. ITE

    AhR agonist

    ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.
  26. (S)-2-Hydroxy-3-phenylpropanoic acid is a product of phenylalanine catabolism. An elevated level of phenyllactic acid is found in body fluids of patients with or phenylketonuria.
  27. platelet PDE inhibitor

    Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
  28. (R)-(+)-Citronellal, isolated from citrus, lavender and eucalyptus oils, is a monoterpenoid and main component of citronellal oil with a distinct lemon scent. A flavouring agent. Used for insect repellent and antifungal properties.
  29. Smilagenin (SMI) is a lipid-soluble small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases.
  30. D-(+)-Phenyllactic acid is an anti-bacterial agent, excreted by Geotrichum candidum, inhibits a range of Gram-positive from humans and foodstuffs and Gram-negative bacteria found in humans.
  31. Mitochondrial respiratory chain inhibitor

    Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain.
  32. DGAT2 inhibitor

    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM.
  33. AHR antagonist

    GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist.
  34. PDE5 inhibitor

    Avanafil is a PDE5 Inhibitor for the Treatment of Erectile Dysfunction
  35. CYP17 inhibitor

    CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
  36. FXR agonist

    Nidufexor is a farnesoid X receptor (FXR) agonist.
  37. (S)-Leucic acid is an amino acid metabolite.
  38. DHFR inhibitor

    Pemetrexed is a novel antifolate with multiple targets
  39. 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.
  40. PDE-4-D inhibitor

    CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
  41. 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.
  42. 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.
  43. 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
  44. Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.
  45. glucokinase activator

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

    Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa.
  48. 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.
  49. 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
  50. 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.

Items 151-200 of 6503

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