Metabolism

Items 1251-1300 of 5815

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  1. Hsp90 inhibitor

    SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM.
  2. LXR agonist

    RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  3. signal transducing G proteins activator

    5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
  4. (S)-(-)-Citronellal ((-)-Citronellal) is a monoterpenoid compound found in Corymbia citriodora and Cymbopogon nardus essential oils.
  5. DGAT1 inhibitor

    DGAT1-IN-1 is a potent DGAT1 inhibitor with IC50 of < 10 nM(cell lysate from Hep3B cells overexpressing human DGAT1).
  6. inosine monophosphate dehydrogenase inhibitor

    Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus.
  7. heme oxygenase 1 (HO-1) inhibitor

    HO-1-IN-1 hydrochloride (Compound 2) is a heme oxygenase 1 (HO-1) inhibitor with an IC50 of 250 nM.
  8. Complex I of oxidative phosphorylation inhibitor

    IACS-010759 Hydrochloride is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
  9. dihydropyrimidine dehydrogenase inhibitor

    Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
  10. dual IDO/TDO inhibitor

    IACS-8968 (R-enantiomer) is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  11. cathepsin K inhibitor

    MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S.
  12. dual IDO/TDO inhibitor

    IACS-8968 (S-enantiomer) is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  13. GK-GKRP disruptor

    AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM.
  14. Adenosine deaminase inhibitor

    EHNA hydrochloride is a specific inhibitor of adenosine deaminase, prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts.
  15. FASN inhibitor

    HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
  16. Desbutyl Lumefantrine D9 is the deuterium labeled euterium labeled, which is a metabolite of Lumefantrine.
  17. Acetoacetic acid sodium salt is a metabolite of non-esterified fatty acids, involved in the development of human diabetes. Acetoacetic acid sodium salt induces oxidative stress to inhibit the assembly of very low density lipoprotein in bovine hepatocytes.
  18. liver CYP3A4 substrate

    Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
  19. MAPKAPK2(MK2) inhibitor

    MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
  20. inhibitor of monoamine oxidase-A (MAO-A)

    Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A).
  21. neuromodulator

    3-Methoxytyramine, a well known extracellular metabolite of 3-hydroxytyramine/dopamine, is a neuromodulator.
  22. Ferroptosis inhibitor

    UAMC-3203 hydrochloride is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM.
  23. Factor XIa (FXIa) inhibitor

    BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.
  24. iron mobilizer

    Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  25. Galactose 1-phosphate Potassium salt is is an intermediate in the galactose metabolism and nucleotide sugars.
  26. HSP inhibitor

    HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
  27. N8-Acetylspermidine dihydrochloride is a polyamine.
  28. GK-GKRP disruptors

    AMG-1694 is a potent glucokinase?Cglucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity.
  29. (3-Carboxypropyl)trimethylammonium chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat.
  30. Pi-Methylimidazoleacetic acid hydrochloride is a potential neurotoxin.
  31. Aldosterone D8 is a deuterium labeled Aldosterone. Aldosterone, produced in the adrenal zona glomerulosa, regulates blood pressure.
  32. PDE9 inhibitor

    BAY 73-6691 racemate is a phosphodiesterase 9 inhibitor extracted from patent WO 2017070293 A1.
  33. Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx).
  34. FXR agonist

    Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.
  35. MAO inhibitor

    Brofaromine (CGP 11305A) is a monoamine oxidase (MAO) inhibitor with IC50 of 0.2?μM for MAO-A.
  36. CRM1 inhibitor

    Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.
  37. FTase inhibitor

    Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
  38. PDE7/GSK3 inhibitor

    VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.
  39. ACC inhibitor

    CP-640186 hydrochloride is a potent and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.
  40. inosine monophosphate dehydrogenase inhibitor

    Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus.
  41. hFAS inhibitor

    GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ?? 4.1 nM in an assay detecting released CoA.
  42. 5-lipoxygenase inhibitor

    Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.
  43. PDE inhibitor

    R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor.
  44. FAAH inhibitor

    FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18??8 nM.
  45. PDE inhibitor

    IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.
  46. CYP450 dependent inhibitor

    Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).
  47. MAO inhibitor

    (S)-Rasagiline (TVP1022) mesylate 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.
  48. LDHA inhibitor

    (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
  49. LDHA inhibitor

    (S)-GNE-140 is the less active enantiomer of GNE-140 which can inhibit Lactate dehydrogenase A (LDHA).
  50. PDE3 inhibitor

    Olprinone(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor.

Items 1251-1300 of 5815

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