Metabolism

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  1. LXR/FXR agonist

    T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively
  2. PPAR agonist

    Rosiglitazone maleate, an antidiabetic drug, works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
  3. FXR agonist

    Cilofexor (GS-9674) is a farnesoid X receptor (FXR) agonist.
  4. FXR agonist

    WAY-362450 is a highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%).

  5. FXR agonist

    GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).
  6. PPARγ agonist

    Troglitazone is a selective PPARγ receptor agonist (EC50 values are 780 and 555 nM at murine and human PPARγ receptors respectively).
  7. PPAR agonist

    Elafibranor is an agonist of the peroxisome proliferator-activated Receptor-α and -δ, induces resolution of nonalcoholic steatohepatitis without fibrosis worsening.
  8. Liver X Receptor Agonist

    GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.
  9. LXR-like receptors agonist

    GW3965 HCl is a selective and orally active liver X receptor (LXR) full agonist.
  10. PPAR agonist

    Rosiglitazone works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
  11. FXR agonist

    Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM
  12. PPARα agonist

    WY 14643 is a highly potent PPARα agonist.
  13. PPAR-α/γ agonist

    Aleglitazar is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.
  14. FXR agonist

    Lithocholic acid is a bile acid that acts as a detergent to solubilize fats for absorption.
  15. ITE

    AhR agonist

    ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.
  16. FXR agonist

    Nidufexor is a farnesoid X receptor (FXR) agonist.
  17. PPARα/γ dual agonist

    Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
  18. RAR agonist

    TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs).
  19. peripheral benzodiazepine receptor agonist

    AC-5216 is a translocator protein [TSPO (18 kDa)] ligand.
  20. PPARδ agonist

    Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1.
  21. PPARδ receptor agonist

    GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.
  22. RARα agonist

    Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.
  23. PPARγ agonist

    Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α.
  24. RARα agonist

    AM 580 is an analog of retinoic acid that acts as a selective RARα agonist.
  25. RARγ-selective agonist

    CD 437 is a synthetic retinoid that is an RARγ-selective agonist.
  26. PPARα agonist

    GW 7647 is a potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively).
  27. PPARδ agonist

    L-165,041 is a potent PPARδ agonist (Ki = 6 nM); displays > 100-fold selectivity for both mouse and human PPARδ receptors over other subtypes.

  28. RAR agonist

    Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo.
  29. RXR agonist

    LG 100268 is a potent RXR agonist for evaluation in the treatment of non-insulin-dependent (type II) diabetes mellitus (NIDDM).
  30. FXR agonist

    LY2562175 is a potent and selective FXR agonist in vitro and has robust lipid modulating properties, lowering LDL and triglycerides while raising HDL in preclinical species.
  31. PPAR agonist

    Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.
  32. PPAR agonist

    Etofylline, also known as BRN-0251760, is a peroxisome proliferator-activated receptor (PPAR) agonist used to treat respiratory and cardiovascular disorders. Etofylline is often used as a bronchodilator.
  33. LXR Inverse Agonist

    SR9238 is a potent and selective LXR inverse agonist (IC50 values are 43 and 214 nM for LXRβ and LXRα, respectively).
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. PPAR agonist

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

    CDDO-Im is a novel synthetic triterpenoid more potent than its parent compound CDDO both in vitro and in vivo; PPARγ Agonist.
  40. PPARα agonist

    Clofibric acid is a PPARα agonist and hypolipidemic agent.
  41. 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.
  42. 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.
  43. FXR anonist

    Tropifexor, also known as LJN452, is a farnesoid X receptor agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
  44. FXR agonist

    PX20606, also known as PX-102, is a FXR agonist. It induces high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice.
  45. FXR agonist

    Px-104, also known as Px-102, is a farnesoid X receptor (FXR) agonist potentially for the treatment of non-alcoholic fatty liver disease.
  46. PPAR agonist

    Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  47. LXR partial agonist

    BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
  48. PPAR-δ agonist

    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
  49. PPARδ agonist

    Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
  50. 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.

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