Metabolism

Items 1951-2000 of 6503

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  1. COX/5-LOX Inhibitor

    Phenethyl ferulate is a potent inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), displaying IC50 values of 4.35 μM and 5.75 μM, respectively. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research into inflammation-related pathways. Its ability to modulate these key enzymes positions it as a promising candidate for studies focused on inflammatory diseases and therapeutic interventions.
  2. 5-LOX/COX Inhibitor

    FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX), exhibiting IC50 values of 3.5 μM and 3.1 μM, respectively, in RBL-1 cells. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory pathways and related diseases. Its dual inhibition of leukotriene and prostaglandin synthesis positions FPL 62064 as a pertinent reagent for studies focusing on inflammation and related therapeutic interventions.
  3. Muscarinic Receptor/Phospholipase C Activator

    (S)-Albuterol is a selective muscarinic receptor agonist that acts as a phospholipase C activator. It is known to elevate intracellular free calcium levels in airway smooth muscle, enhancing muscle contraction. This compound is widely utilized in research applications focusing on airway physiology and the mechanisms underlying bronchoconstriction.
  4. Drug metabolite

    SCH-720881 is the active metabolite of Rolapitant, a selective and long-acting neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. This compound exhibits significant anti-emetic properties, making it valuable for studies involving nausea and vomiting. SCH-720881 provides insights into the pharmacological effects of NK1 receptor modulation in various preclinical models, thereby facilitating research into anti-emetic therapies.
  5. Fungal Secondary Metabolite

    Benzomalvin B is a fungal secondary metabolite that serves as a less active analog of Benzomalvin A. It exhibits weak activity against substance P, making it a compound of interest for research into neuropeptide signaling and related biological processes. Its properties may facilitate studies in pain modulation and the exploration of therapeutic avenues in neurobiology.
  6. oral iron chelator

    CGP 65015 is an oral iron chelator, which can mobilize iron deposits.
  7. APT-2 inhibitor

    ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
  8. CYP3A4 enzyme inhibitor

    Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
  9. p32-kinase activator

    D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
  10. δ6 desaturase inhibitor

    Selective δ6 desaturase inhibitor (IC50 = 0.2 μM in vitro).
  11. Carbonic anhydrase inhbitor

    Indisulam (E7070) is a carbonic anhydrase inhbitor, is also a novel synthetic sulfon-amide that targets the G1 phase of the cell cycle.
  12. Indole-3-carboxylic acid is a normal urinary indolic tryptophan metabolite and has been found elevated in patients with liver diseases.
  13. FOXO relocator

    LOM612 is a potent FOXO relocator, with an EC50 value of 1.5 μM in cells.
  14. PPARα agonist

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

    Dehydroascorbic acid, a blood-brain barrier transportable form of vitamin C, mediates potent cerebroprotection in experimental stroke.
  16. 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.
  17. GAPDH inhibitor

    CGP 3466B maleate is an orally active glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor.
  18. 4-Pyridoxic acid is a catabolic product of vitamin B6 which is excreted in the urine.
  19. 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.
  20. PPAR antagonist

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

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

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

    Brequinar is an inhibitor of dihydroorotate dehydrogenase, an enzyme that is required for de novo pyrimidine biosynthesis.
  26. 5-LPO inhibitor

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

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

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

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

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

    CHS-828 is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM.
  32. 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.
  33. 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.
  34. 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).
  35. FXR agonist

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

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

    PKR-IN-2 is a pyruvate kinase (PKR) activator.
  38. 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.
  39. (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.
  40. platelet PDE inhibitor

    Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
  41. (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.
  42. 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.
  43. 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.
  44. 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.
  45. DGAT2 inhibitor

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

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

    Avanafil is a PDE5 Inhibitor for the Treatment of Erectile Dysfunction
  48. 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.
  49. FXR agonist

    Nidufexor is a farnesoid X receptor (FXR) agonist.
  50. (S)-Leucic acid is an amino acid metabolite.

Items 1951-2000 of 6503

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