Metabolism

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  1. ALDH2 inhibitor

    RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
  2. IDH1 inhibitor

    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ?? 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
  3. ETC inhibitor

    MitoTam bromide, hydrobromide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology.
  4. NAPE-PLD inhibitor

    ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor with an IC50 of ~34 μM.
  5. autotaxin inhibitor

    Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain.
  6. Autotaxin inhibitor

    PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model.
  7. SCD1 inhibitor

    SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor.
  8. prolyl hydroxylase inhibitor

    Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia.
  9. PFKFB3 inhibitor

    KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 0.19 μM .
  10. carbonic anhydrase inhibitor

    Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic drug.
  11. SHMT1/2 inhibitor

    SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay.
  12. PGS inhibitor

    PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
  13. PFKFB3 inhibitor

    AZ PFKFB3 26 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 23 nM. AZ PFKFB3 26 inhibits PFKFB1 and PFKFB2 with IC50s of 2.06 and 0.384 μM, respectively.
  14. cPLA2 and iPLA2 inhibitor

    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
  15. fungal Cyp51 inhibitor

    Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
  16. ATX inhibitor

    Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.
  17. Hsp90 inhibitor

    KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.
  18. 5-lipoxygenase inhibitor

    LY 178002 is a potent inhibitor of 5-lipoxygenase, phospholipase A2, with IC50 of 0.6 μM for 5-1ipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
  19. monoamine oxidase-A inhibitor

    2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
  20. PDE5 inhibitor

    Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  21. ACE inhibitor

    NCX899 is a NO-releasing derivative of enalapril, and shows inhibitory activity against angiotensin-converting enzyme (ACE) activity.
  22. TYK2 inhibitor

    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively.
  23. MPC inhibitor

    MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects.
  24. PAI-1 inhibitor

    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines.
  25. IDO inhibitor

    IDO-IN-11 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.18 μM (Kinase) and 0.014 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 13.
  26. FASN inhibitor

    FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme.
  27. s-EH inhibitor

    AR9281 is a potent and selective inhibitor of soluble epoxide hydrolase (s-EH), with potential for the treatment of hypertension and type 2 diabetes.
  28. 5-LO inhibitor

    A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO).
  29. Cholesterol biosynthesis inhibitor

    Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.
  30. Cytochrome P450 inhibitor

    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
  31. PDE-4 inhibitor

    WAY127093B racemate is the racemate of WAY127093B. WAY127093B is a novel, orallyactive phosphodiesterase IV inhibitor in guinea pigs and rats.
  32. IDO1 inhibitor

    LY-3381916 is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  33. LDH inhibitor

    LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively.
  34. IDH1 inhibitor

    IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H.
  35. 5-lipoxygenase inhibitor

    Esculetin, a phenolic compound, acts as a 5-LO (5-lipoxygenase, 5-LOX) inhibitor.
  36. alpha-glucosidase inhibitor

    Voglibose is an N-substituted derivative of valiolamine, excellent inhibitory activity against alpha-glucosidases and its action against hyperglycemia and various disorders caused by hyperglycemia.
  37. Carbonic anhydrase (CA) inhibitor

    U-104 is a novel ureido-sulfonamide inhibitor of Carbonic Anhydrase IX (CAIX).
  38. Factor Xa inhibitor

    5-R-Rivaroxaban is (R) enantiomer of Rivaroxaban. Rivaroxaban is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders.
  39. DGAT-1 inhibitor

    ABT-046 is a potent, selective, and orally bioavailable Diacylglycerol acyltransferase 1 (DGAT-1 ) inhibitor (IC50= 8 nM).
  40. Hsp90 inhibitor

    Alvespimycin is a selective Hsp90 inhibitor with a GI50 of 53 nM.
  41. CYP3A4 Inhibitor

    Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA.
  42. DGAT1 inhibitor

    AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1).
  43. CYP2C19/CYP2B6 inhibitor

    Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.
  44. DGAT-1 inhibitor

    DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.
  45. Factor Xa inhibitor

    Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.
  46. SGK inhibitor

    EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 uM.
  47. PDE Inhibitor

    GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.
  48. Liver-targeting SCD Inhibitor

    MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
  49. lipoxygenase inhibitor

    Nordihydroguaiaretic acid is a natural phenolic compound isolated from the creosote bush Larrea divaricata, which has anti-tumor activities both in vitro and in vivo. Its analogs are in clinical development for use in refractory solid tumors.
  50. PDE5 inhibitor

    Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.

Items 551-600 of 2992

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