Retinoid Receptor

Retinoid receptor ligands act on retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Both are nuclear receptors with α, β and γ subtypes that bind DNA as RAR-RXR heterodimers and regulate gene transcription. A receptor for the morphogen retinoic acid was identified in 1987 as a member of the nuclear receptor family. In 1990 a second receptor responding to retinoic acid, later named RXRα, revealed a distinct retinoid pathway. Tretinoin, the all-trans form of retinoic acid, activates RARs, while tamibarotene and AM 580 favor RARα and CD 437 favors RARγ. Adapalene, tazarotene, acitretin and fenretinide are synthetic retinoids, whereas bexarotene is a ligand selective for RXRs.

3 Items

  • LG100754
    Cat. No.
    A77461

    LG100754

    Synonyms: UVI 2112

    LG100754 is an RXR modulator that functions as an antagonist of RXR:RXR homodimers while acting as an agonist for RXR:PPARα and RXR:PPARγ heterodimers. This compound serves as an insulin sensitizer, exerting its biological effects through receptor interactions involving the retinoid X receptor (RXR). Its unique modulation of RXR dimers makes LG100754 a valuable tool for research in metabolic disorders and cellular signaling pathways.

    5 mg
    $100.00
    10 mg
    $160.00
    All 5 sizes
  • RXR antagonist 1
    Cat. No.
    A77472

    RXR antagonist 1

    RXR Antagonist 1 is a selective retinoid X receptor (RXR) modulator demonstrating potent antagonistic activity, with a pA2 value of 8.06. This compound is particularly relevant in research pertaining to type 2 diabetes, offering insights into RXR-related pathways and their impact on metabolic processes. Its effective inhibition of RXR activity makes it a valuable tool for exploring therapeutic interventions in metabolic disorders.

    5 mg
    $420.00
    10 mg
    $685.00
    All 5 sizes
  • LG101506
    Cat. No.
    A77487

    LG101506

    LG101506 is a selective and orally active retinoid X receptor (RXR) modulator that exhibits a Ki of 2.7 nM for RXRα. This compound has demonstrated potential in research applications related to type 2 diabetes and cancer, making it a valuable tool for studying RXR's role in metabolic and oncological pathways.

    5 mg
    $760.00
    10 mg
    $1,165.00
    All 5 sizes

3 Items

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