Retinoid Receptor

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  1. Acitretin is a second generation retinoid and is typically used for psoriasis.
  2. Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions.
  3. Tazarotene is a prodrug and a member of the acetylenic class of retinoids.
  4. RAR agonist

    Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors).
  5. Retinoid X Receptor Ligand

    Bexarotene is a highly selective retinoid X receptor (RXR) agonist.
  6. 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.
  7. 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.
  8. RARα agonist

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

    CD 437 is a synthetic retinoid that is an RARγ-selective agonist.
  10. RAR agonist

    Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo.
  11. Palovarotene is a novel retinoic acid receptor gamma agonist for the treatment of emphysema
  12. RARα antagonist.

    AR7 was developed as a highly potent and selective enhancer of the chaperone-mediated autophagy (CMA) through antagonizing RARα.
  13. RAR agonist

    TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs).
  14. RXR agonist

    LG 100268 is a potent RXR agonist for evaluation in the treatment of non-insulin-dependent (type II) diabetes mellitus (NIDDM).
  15. 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.
  16. 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.
  17. 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).
  18. 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.
  19. 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.
  20. Etretinate is a second-generation retinoid to treat severe psoriasis; has been replaced by acitretin, a safer metabolite of etretinate.
  21. RAR agonist

    WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist.
  22. antagonist of RXRα

    β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
  23. RXR agonist

    LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
  24. RAR degrader

    PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader.
  25. RARγ antagonist

    LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.
  26. RXR antagonist

    UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
  27. Human RARβ2 receptor agonist

    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
  28. RARα agonist

    AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
  29. RAR agonist

    Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
  30. RXRα antagonist

    β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
  31. RARβ agonist

    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist.

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