Metabolism

Items 601-650 of 5815

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  1. Eflornithine hydrochloride, hydrate is a drug found to be effective in the treatment of facial hirsutism.
  2. 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.
  3. Pyridoxamine is one form of vitamin B6. Chemically it is based on a pyridine ring structure, with hydroxyl, methyl, aminomethyl, and hydroxymethyl substituents.
  4. CYP2C9 inhibitor

    Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
  5. pan-WNK-kinase inhibitor

    WNK463 is an orally bioavailable pan-WNK-kinase inhibitor.
  6. 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.
  7. oxidative phosphorylation blocker

    Imeglimin is an oxidative phosphorylation blocker that acts to inhibit hepatic gluconeogenesis, increase muscle glucose uptake, and restore normal insulin secretion.
  8. oxidative phosphorylation blocker

    Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins. It has been shown to act on the liver, muscle and pancreatic ??-cells to uniquely target the key defects of type 2 diabetes.
  9. 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.
  10. 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.
  11. 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).
  12. 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.
  13. 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.
  14. 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.
  15. PPAR agonist

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

    CDDO-Im is a novel synthetic triterpenoid more potent than its parent compound CDDO both in vitro and in vivo; PPARγ Agonist.
  17. 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.
  18. glucokinase activator

    AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
  19. 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.
  20. SINE/CRM1 inhibitor

    KPT276, analog of KPT-185, is a selective inhibitor of nuclear export (SINE) and CRM1.
  21. HSF inhibitor

    KRIBB11 is an inhibitor of Heat shock factor (HSF) inhibitor, with IC50 of 1.2 μM.
  22. Etretinate is a second-generation retinoid to treat severe psoriasis; has been replaced by acitretin, a safer metabolite of etretinate.
  23. MGL inhibitor

    URB602 is a selective inhibitor of monoglycerol lipase (MGL), exhibiting an IC50 of 28 μM for the rat brain enzyme.
  24. Thiamin antagonist

    Amprolium chloride is a thiamin antagonist, which prevents carbohydrate synthesis by blocking thiamine uptake.
  25. Tryptophan hydroxylase inhibitor

    4-Chloro-DL-phenylalanine is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE).
  26. Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.
  27. Choline bitartrate is a form of the nutrient choline which is found in foods.
  28. Choline chloride is a quaternary ammonium salt used as an additive for animal feed.
  29. Clofazimine is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2.
  30. PPARα agonist

    Clofibric acid is a PPARα agonist and hypolipidemic agent.
  31. glucose metabolism inhibitor

    2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.
  32. iron-chelating drug

    Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload.
  33. Deoxycorticosterone acetate (DOCA) is a corticosteroid.
  34. Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.
  35. OXPHOS Uncoupler

    FCCP is an ionophore that is a mobile ion carrier. It is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.
  36. α-glucosidase inhibitor

    Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
  37. excitatory transmitter/agonist

    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  38. ferroptosis inhibitor

    Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC50=22 nM).
  39. Impulsin (AM 3112) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.
  40. PPARγ agonist

    Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  41. COX-2 inhibitor

    Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.
  42. Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  43. Sucralose is an activator of taste receptor, type 1, member 2 (T1R2) and taste receptor type 1, member 3 (T1R3).
  44. Vitamin D2 (Ergocalciferol) is a form of vitamin D, used as a vitamin D supplement.
  45. diacylglycerol lipase (DAGL) inhibitor

    DO34 is a novel potent and selective diacylglycerol lipase (DAGL) inhibitor.
  46. ACE2 inhibitor

    MLN-4760 is an angiotensin-converting (ACE2) inhibitor. In huMNCs, MLN-4760-B detected 63% ACE2 with 28-fold selectivity over ACE.
  47. sEH inhibitor

    UC-1728, also known as t-TUCB, is a soluble epoxide hydrolase inhibitor.
  48. CYP1A1 inhibitor

    Bergamottin is a furanocoumarin found in grapefruit juice and lemon, lime, and bergamot oils that has diverse biological activities.
  49. IDH1 Inhibitor

    Vorasidenib, also known as AG-881, is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity.
  50. LOXL2 inhibitor

    LOXL2-IN-1 HCl is a selective LOXL2 inhibitor with an IC50 of 126 nM.

Items 601-650 of 5815

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