Metabolism

Items 2051-2100 of 6503

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  1. Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor

    Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM.
  2. PPARδ agonist

    Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1.
  3. biomarker

    N6-Etheno 2'-deoxyadenosine is a reactive oxygen species (ROS)/reactive nitrogen species (RNS)-induced DNA oxidation product, used as a biomarker to evaluate chronic inflammation and lipid peroxidation in animal or human tissues.
  4. PDE5 inhibitor

    Udenafil is a PDE5 inhibitor used in urology to treat erectile dysfunction.
  5. MAO-B inhibitor

    Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration.
  6. SCD1 inhibitor

    A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
  7. Anserine is a dipeptide found in skeletal muscle of vertebrates.
  8. PDE3 inhibitor

    Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
  9. Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  10. NAMPT Inhibitor

    GNE-617 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with IC50 value of 5nM.
  11. LDHA Inhibitor

    AZ33 is a LDHA Inhibitor.
  12. leukotriene biosynthesis inhibitor

    MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
  13. 15-LO inhibitor

    PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis.
  14. MAO Inhibitor

    Bifemelane hydrochloride is an antidepressant MAO inhibitor. Reverses catalepsy induced by tetrabenazine in mice and increases locomotor activity in MPTP-treated marmosets.
  15. LSD1/BHC110 & MAO inhibitor

    Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor.
  16. ABT

    Cytochrome P450 inhibitor

    ABT (1-Aminobenzotriazole )is a suicide substrate for (CYP)cytochrome P-450 and chloroperoxidase.
  17. Fluorescent P450 substrate

    3-Cyano-7-ethoxycoumarin is a fluorogenic substrate suitable for the continuous determination of cytochrome P450 mixed-function monooxygenases. It is a fluorescent probe useful in microsomal dealkylase studies.
  18. CYP2C19 and CYP2B6 substrate

    Mephenytoin is a CYP2C19 substrate. Anticonvulsant.
  19. cytochrome P450 substrate

    Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes.
  20. HMG-CoA reductase inhibitor

    Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease.
  21. Peroxisome Proliferator

    Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology.
  22. CYP17 inhibitor

    TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.
  23. FAAH Inhibitor

    PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It reduces inflammatory pain via a cannabinoid receptor-dependent mechanism.

  24. HMG-CoA Reductase inhibitor

    Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.

  25. PDE10A inhibitor

    PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.

  26. CETP inhibitor

    JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis.
  27. CETP inhibitor

    Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM.
  28. Cathepsin K Inhibitor

    Odanacatib is an inhibitor of cathepsin K,an enzyme involved in bone resorption.
  29. Hsp90 inhibitor

    IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).
  30. HSP90 inhibitor

    IPI-493 is a potent and orally bioavailable HSP90 inhibitor with Ki of 21 nM.
  31. CYP3A Inhibitor

    Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate.
  32. Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.
  33. ACE inhibitor/Beta blocker

    Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction.
  34. PDE-2 Inhibitor

    BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human).
  35. Calcipotriol is a low-calcemic vitamin D receptor (VDR) agonist.
  36. Calcifediol is a major circulating metabolite of vitamin D3 and acts as a competitive inhibitor with an apparent Ki of 3.9 μM. It also suppresses PTH secretion and mRNA (ED50=2 nM)
  37. Collagen proline hydroxylase inhibitor

    Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor.
  38. DGAT1 inhibitor

    T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
  39. PC-PLC inhibitor

    D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.
  40. SGK1 inhibitor

    EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  41. SGK1 inhibitor

    EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  42. Androgen Receptor antagonist

    Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity.
  43. Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.
  44. PPARδ receptor agonist

    GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.
  45. Cathepsin Inhibitor

    Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
  46. TPH inhibitor

    LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
  47. Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.
  48. Vitamin D Analog

    Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays.
  49. DHFR inhibitor

    Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.
  50. DGAT1 Inhibitor

    PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

Items 2051-2100 of 6503

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