Metabolism

Items 1101-1150 of 5815

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  1. dual FXR and GPBAR1 agonist

    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  2. STK16 kinase inhibitor

    STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.
  3. RAR agonist

    Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
  4. plasminogen activator inhibitor

    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
  5. (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
  6. fumarate hydratase inhibitor

    Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM.
  7. GPX4 inhibitor

    ML-210??the most potent compound in the nitroisoxazole series?? is a selective covalent inhibitor of glutathione peroxidase 4 (GPX4) by binding the selenocysteine residue.
  8. SCD1 inhibitor

    XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.
  9. NO synthase inhibitor

    Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
  10. PDE4 inhibitor

    CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
  11. Diethylphosphate (DEP) is product of metabolism and of environmental degradation of a commonly used insecticide Chlorpyrifos.
  12. Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
  13. aldosterone synthase inhibitor

    BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
  14. Coenzyme Q9, a nine isoprenyl group-containing member of the ubiquinone family, is a normal constituent of human plasma.
  15. AhR activator

    Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
  16. mPTP opening inhibitor

    ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8?μM.
  17. Iberin is a sulforaphane homolog and antioxidant. It induces phase II enzyme activity and suppresses CDK expression, inducing apoptosis in cancer cells.
  18. 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is a modified nucleoside. 2-(Methylamino)-1H-purin-6(7H)-one is an endogenous methylated nucleoside found in human fluids.
  19. PDE inhibitor

    ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
  20. 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric acid (GABA) derivative.
  21. uPA system inhibitor

    UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system.
  22. NOS inhibitor

    SDMA (Symmetric dimethylarginine) is an endogenous inhibitor of nitric oxide (NO) synthase activity.
  23. IDO inhibitor

    IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
  24. O-Acetylserine (O-Acetyl-L-serine) is an intermediate in the biosynthesis of the amino acid cysteine in bacteria and plants.
  25. FAAH inhibitor

    FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.
  26. NMDA receptor antagonist

    Docosatrienoic acid is a rare ??-3 fatty acid; inhibits LTB4 binding to pig neutrophil membranes with an Ki of 5 μM.
  27. Glyoxalic acid (NSC 27785) is an organic compound that is both an aldehyde and a carboxylic acid.
  28. DL-Homocysteine thiolactone hydrochloride is a cyclic amino acid derivative that exhibits root-growth inhibitory activity.
  29. NF-κB inhibitor

    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation.
  30. γ-Glu-Phe is a γ-3 glutamyl dipeptide found in sourdough.
  31. Coproporphyrin III is a porphyrin derivative.
  32. Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.
  33. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
  34. Hypotaurine (2-aminoethanesulfinic acid), an intermediate in taurine biosynthesis from cysteine in astrocytes, is an endogenous inhibitory amino acid of the glycine receptor.
  35. TPH1 Inhibitor

    Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH).
  36. hexokinase II inhibitor

    3-Bromopyruvic acid is a hexokinase II inhibitor, is an effective antitumor agent on the hepatoma cells.
  37. Asparagusic acid (1,2-dithiolane-4-carboxylic acid) is unique to asparagus. The compound is responsible for the odorous urine excreted after eating asparagus. Its derivatives ihydroasparagusic acid have anti-inflammatory effect.
  38. GMP inhibitor

    3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
  39. L-Pyroglutamic acid is the levo-isomer of Pyroglutamic acid. L-Pyroglutamic acid is the biologically active enantiomer in humans. Pyroglutamic acid is an intermediate in glutathione metabolism.
  40. Wnt/β-catenin activator

    Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
  41. PPAR agonist

    Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  42. LXR partial agonist

    BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
  43. PDE10A inhibitor

    Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.
  44. anti-secretagogue of PCSK9

    R-IMPP is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
  45. recombinant human sEH inhibitor

    GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.
  46. COX-2/5-LO inhibitor

    S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
  47. PDE3 inhibitor

    NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
  48. IDH1 mutant inhibitor

    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  49. SAH

    METTL3-14 inhibitor

    SAH is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 ?M.
  50. PPAR-δ agonist

    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.

Items 1101-1150 of 5815

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