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Transthyretin (TTR)

Transthyretin (TTR) stabilizers and related ligands act on a plasma carrier of thyroxine and retinol. TTR circulates as a tetramer that binds thyroxine and, through retinol-binding protein 4 (RBP4), carries vitamin A. Dissociation of the tetramer into monomers is the rate-limiting step for misfolding into amyloid fibrils. In 2003 stabilization of the tetramer was shown to prevent this process in transthyretin amyloid disease. Tafamidis and tafamidis meglumine bind the thyroxine sites and act as kinetic stabilizers. Patisiran sodium is a small interfering RNA (siRNA) that lowers TTR synthesis. A 1120, an RBP4 ligand, was reported in 2009 to lower serum RBP4 levels in mice. Tinlarebant and STG-001 are listed as further antagonists of the same retinol carrier.

1 Item

  • RBP4 ligand-1
    Cat. No.
    A75935
    CAS No.
    260553-24-0

    RBP4 ligand-1

    RBP4 ligand-1 is a synthetic non-retinoid ligand that specifically targets retinol-binding protein 4 (RBP4). This compound exhibits significant binding affinity, with an IC50 value of 0.23±0.11 μM in the radioligand binding assay and 0.13±0.12 μM in the RBP4-thyroxine transport receptor (TTR) Förster resonance energy transfer (FRET) assay. RBP4 ligand-1 is valuable for research applications aimed at understanding RBP4-related pathways and its implications in metabolic diseases.

    In stock View Details
    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

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