Metabolism

Items 2351-2400 of 6503

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  1. MAO inhibitor

    Olodaterol is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim.
  2. LXR Inverse Agonist

    SR9238 is a potent and selective LXR inverse agonist (IC50 values are 43 and 214 nM for LXRβ and LXRα, respectively).
  3. PCSK9 antagonist

    SBC-115076 is an anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds, for the treatment and/or prevention of cardiovascular diseases.
  4. FPTase inhibitor

    L-778123 HCl is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.
  5. 15-PGDH enzyme inhibitor

    SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.
  6. PDE10A inhibitor?€?

    TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
  7. ACL inhibitor and AMPK activator

    ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
  8. cytochrome P450 inhibitor

    Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
  9. PPAR agonist

    BMS-687453 is a potent and selective peroxisome proliferator activated receptor (PPAR) alpha agonist, with an EC(50) of 10 nM for human PPARalpha and approximately 410-fold selectivity vs human PPARgamma in PPAR-GAL4 transactivation assays.
  10. Carbonic Anhydrase Inhibitor

    Acetazolamide, a potent carbonic anhydrase (CA) inhibitor, is commonly used in clinical practice as an immediate and readily available option for acute reduction of intraocular pressure(IOP).
  11. Dehydrogenase Inhibitor

    AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
  12. Glucose Transporter Inhibitor I

    WZB117 is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 uM.
  13. hALDH1 Inhibitor

    NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
  14. PKM2 Activator

    DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
  15. Calcium D-Panthotenate is a water-soluble vitamin and an essential nutrient for many animals.
  16. STK33 inhibitor

    ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.
  17. lipase inhibitor

    Cetilistat is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine.
  18. FAAH inhibitor

    JNJ-42165279 is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor.
  19. Lometrexol is a folate analog antimetabolite with antineoplastic activity.
  20. broad spectrum antimetabolite

    LY2334737 is an orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity.
  21. Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.
  22. TPPII inhibitor

    Butabindide oxalate is a selective and potent inhibitor of TPPII (tripeptidyl peptidase II).
  23. HSP90 inhibitor

    Gedunin, a naturally occurring Hsp90 inhibitor, is tetranortriterpenoid isolated from the Indian neem tree (Azadirachta indica).
  24. HSP90 inhibitor

    Macbecin I is an ansamycin antibiotic compound that inhibits Hsp90 activity with IC50 value of μM by binding to the ATP-binding site.
  25. HSP70 inducer

    TRC 051384, belonging to substituted 2-propen-1-one class, is a potent inducer of heat shock protein 70 (HSP70) [1]. Induction of HSP70 is a natural response of stressed cells that protects neuronal cells from a variety of insults including acute ischemia.
  26. HSP90 inhibitor

    EC 144 is a potent inhibitor of the heat shock protein 90 and was found to be effective in tumor growth suppression.
  27. FXR antagonist

    DY 268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM).
  28. SINE inhibitor

    KPT 335 is an orally bioavailable Selective Inhibitor of Nuclear Export (SINE).
  29. MAGL inhibitor

    MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA).
  30. SREBP inhibitor

    Fatostatin Hydrobromide is an inhibitor of sterol regulatory element-binding protein (SREBP).
  31. PDI inhibitor

    CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.
  32. PDE5 inhibitor

    Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
  33. alcohol dehydrogenase inhibitor

    Fomepizole is an alcohol dehydrogenase inhibitor used for the treatment of ethylene glycol and methanol poisonings in adults.
  34. Eflornithine hydrochloride, hydrate is a drug found to be effective in the treatment of facial hirsutism.
  35. PHGDH inhibitor

    CBR 5884 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 33 uM.
  36. Pyridoxamine is one form of vitamin B6. Chemically it is based on a pyridine ring structure, with hydroxyl, methyl, aminomethyl, and hydroxymethyl substituents.
  37. CYP2C9 inhibitor

    Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
  38. PKM2 activator

    TEPP-46 is a potent and selective activator of recombinant pyruvate kinase M2 (PKM2) with half-maximum activating concentration (AC50 value) of 92 nM, and little or no activity versus PKM1, PKL and PKR.
  39. oxidative phosphorylation blocker

    Imeglimin is an oxidative phosphorylation blocker that acts to inhibit hepatic gluconeogenesis, increase muscle glucose uptake, and restore normal insulin secretion.
  40. pan-RARs agonist

    AGN 194310 is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.
  41. RARα agonist

    AGN 195183 is a potent and selective agonist of RARα (Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.
  42. RARα antagonist

    AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
  43. RAR agonist

    AGN 205327 is a potent synthetic RARs agonist with EC50 of 3766/734/32 nM for RARα/β/γ respectively; no inhibition on RXR.
  44. RARγ antagonist

    AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.
  45. ribonucleotide reductase inhibitor

    Didox is a strong inhibitor of ribonucleotide reductase (RR) that interferes with DNA synthesis and repair by blocking the production of deoxyribonucleotides and has demonstrated antitumor effects for decades.
  46. PPAR agonist

    Bezafibrate is the first clinically tested dual and pan-PPAR co-agonist.
  47. PPARγ Agonist

    CDDO-Im is a novel synthetic triterpenoid more potent than its parent compound CDDO both in vitro and in vivo; PPARγ Agonist.
  48. PPARβ/δ inverse agonist

    DG-172 is an orally active potent PPARβ/δ inverse agonist (IC50 = 26.9 nM). DG-172 inhibits Angptl4 gene expression in mouse myoblasts (IC50 = 9.5 nM) in vitro.
  49. glucokinase activator

    AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
  50. LYPLA1 inhibitor

    ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.

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