Metabolism

Items 701-749 of 6503

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  1. Artefenomel (OZ439) is a synthetic antimalarial agent with the artemisinin pharmacophore. Artefenomel (OZ439) is a long-acting artemisinin-related agent.
  2. ACE/NEP inhibitor

    Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.
  3. L-CPT1 inhibitor

    Teglicar is a selective and reversible inhibitor of liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1).
  4. angiotensin-converting enzyme inhibitor

    Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
  5. IDO inhibitor

    IDO-IN-5 (NLG-1489) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1489, has an IC50 of 1-10 μM.
  6. Cyhalofop(Cyhalofop acid) is a recently registered herbicide from the aryloxyphenoxy propionate group in India to control a wide range of grass weed species at various growth stages in rice crop.
  7. IDO-1 inhibitor

    IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor, extracted from patent WO2014150677A1, Compound example 1 enantiomer 1.
  8. 11β-HSD1 inhibitor

    AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
  9. ACLY inhibitor

    SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
  10. CYP26 inhibitor/RAMBA

    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  11. PPARγ agonist

    Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
  12. Afegostat is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with high affinity.
  13. VD3-D6(Vitamin D3-26,26,26,27,27,27-d6) is the deuterated form of Vitamin D3; tools for determination of Vitamin D3 metabolites in human serum.
  14. PPAR agonist

    Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).
  15. mutant IDH1 R132H inhibitor

    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
  16. Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitic C virus and intracellular bacterial infections.
  17. SREBP activation inhibitor

    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2.
  18. HO inhibitor

    Tin(IV) mesoporphyrin IX dichloride (Stannsoporfin) is a heme oxygenase (HO) inhibitor being developed for the prevention of hyperbilirubinemia in infants at risk of developing jaundice, extracted from patent WO2011103196A1.
  19. L-Theanine (L-Glutamic Acid ??-ethyl amide??is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities.
  20. chemoprotective agent

    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
  21. Hsc70 and Hsp70 inhibitor

    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14?μM, respectively, and can induce apoptosis.
  22. Olesoxime (TRO 19622) is a mitochondrial-targeted neuroprotective compound with mean EC50 value for increasing cell survival is 3.2??0.2 ?M.
  23. PPARγ agonist

    Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
  24. Miquelianin is one of the flavonoids of St. John's wort (Hypericum perforatum L.) with antidepressant activity.
  25. Nampt inhibitor

    CB30865(ZM 242421) is a potent inhibitor of Nampt , an enzyme present in the NAD biosynthetic pathway.
  26. PDE4D inhibitor

    D159687 is a selective PDE4D inhibitor.
  27. HMG-CoA reductase inhibitor

    Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
  28. MAO-A inhibitor

    RS 8359 is a selective and reversible MAO-A inhibitor, with antidepressant activity.
  29. PDE8 inhibitor

    PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.
  30. PDE-5 inhibitor

    Mirodenafil(SK3530) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
  31. cholesterol biosynthesis inhibitor

    Lapaquistat (T-91485), a cholesterol biosynthesis inhibitor, is the active metabolite of TAK-475. Lapaquistat can decrease statin-induced myotoxicity in lipid-lowering therapy.
  32. MAO-B inhibitor

    Lazabemide(Ro 19-6327) is selective, reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).
  33. MAO-B inhibitor

    (S)-Rasagiline (TVP1022) is the S-isomer of Rasagiline, which is an anti-Parkinson drug, appears to have the same neuroprotective activity as the R-isomer, but is 1000-fold less active as an MAO-B inhibitor.
  34. Cholecalciferol(Vitamin D3) is a naturally occuring form of vitamin D; Reported that upon metabolic activation, Cholecalciferol induces cell differentiation and prevents proliferation of cancer cells.
  35. steroid sulfatase inhibitor

    Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
  36. FAAH inhibitor

    PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme??s active site serine nucleophile.
  37. FAAH/Carbamate inhibitor

    SA 47 is a selective and potent inhibitor of fatty acid amide hydrolase (FAAH) and carbamate.
  38. Dehydrogenases substrate

    Nitro blue tetrazolium chloride (NBT) is a substrate for dehydrogenases; is used with the alkaline phosphatase substrate 5-Bromo-4-Chloro-3-Indolyl Phosphate (BCIP) in western blotting and immunohistological staining procedures.
  39. 11β-HSD1 inhibitor

    PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells).
  40. 11β-HSD1 inhibitor

    BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
  41. IDH inhibitor

    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
  42. 11β-HSD1 inhibitor

    BVT 2733 is a new, small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
  43. DGAT2 inhibitor

    PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM.
  44. Monoamine oxidase inhibitor

    Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible inhibitor of monoamine oxidase.
  45. mutant-selective IDH1 inhibitor

    Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
  46. LXRα and full LXRβ agonist

    LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
  47. NAMPT inhibitor

    Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
  48. GK activator

    Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.

  49. PDE3 inhibitor

    Saterinone hydrochloride is a phosphodiesterase III (PDE III) inhibitor.

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