Metabolism

Items 1151-1200 of 5815

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  1. MAGL inhibitor

    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.
  2. cholesterol solubilizer

    Aramchol, also known as Arachidyl amido cholanoic acid, is a cholesterol solubilizer that prevents gallstone formation in inbred mice. Aramchol reduces liver fat content in patients with nonalcoholic fatty liver disease.
  3. Heme oxygenase (HO)-1 inducer

    Hemin is an iron-containing porphyrin. Hemin is an Heme oxygenase (HO)-1 inducer.
  4. IDO inhibitor

    IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.
  5. IDO-1 inhibitor

    PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.
  6. PTP1B/IKK-βinhibitor and dual PPARα and PPARβ agonist

    Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
  7. SCD inhibitor

    GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16.
  8. allosteric glucokinase activator

    MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.
  9. FASN inhibitor

    Desoxyrhaponticin is a stilbene glycoside from the Tibetan nutritional food Rheum tanguticum Maxim. Desoxyrhaponticin is a Fatty acid synthase (FAS) inhibitor, and has apoptotic effect on human cancer cells.
  10. CYP51 inhibitor

    Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51.
  11. ACC inhibitor

    Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
  12. SREBP inhibitor

    Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.
  13. PPARδ agonist

    Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
  14. PFT inhibitor

    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
  15. phospholipase A2 inhibitor

    Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
  16. PPAR alpha/gamma agonist

    Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively.
  17. Small utrophin's translation modulator

    Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
  18. IDO inhibitor

    IDO-IN-3 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 290 nM.
  19. LDHA inhibitor

    FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell??a Ki value of 8 μM.
  20. SREBP inhibitor

    FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.
  21. DAF-9 cytochrome P450 inhibitor

    Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
  22. SGK-1 inhibitor

    SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
  23. Farnesyl transferase inhibitor

    BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
  24. SCD1 inhibitor

    MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an EC50 of 2.3 nM for rSCD1.
  25. Arglabin is a sesquiterpene gamma-lactone is isolated from Artemisia glabella; anticancer natural compound.
  26. nuclear export receptor CRM1 inhibitor

    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
  27. HSP90α/HSP90β inhibitor

    TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
  28. Heparin is a highly sulfated glycosaminoglycan,that is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule.
  29. 2'-Deoxycytidine hydrochloride is composed of the purine nucleoside guanine linked by its N9 nitrogen to the C1 carbon of deoxyribose.
  30. CYP17 lyase inhibitor

    Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
  31. ACC inhibitor

    Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
  32. CYP3A4/5 inhibitor and substrate

    Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  33. Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
  34. LXR agonist

    AZ876 is a novel high-affinity LXR agonist.
  35. Artefenomel (OZ439) is a synthetic antimalarial agent with the artemisinin pharmacophore. Artefenomel (OZ439) is a long-acting artemisinin-related agent.
  36. 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.
  37. L-CPT1 inhibitor

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

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

    VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. ACLY inhibitor

    SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
  45. 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.
  46. 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.
  47. Afegostat is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with high affinity.
  48. 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.
  49. 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).
  50. mutant IDH1 R132H inhibitor

    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

Items 1151-1200 of 5815

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