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Thyrotropin Receptor (TSHR)

Thyrotropin receptor (TSHR) agonists and antagonists act on the receptor for thyroid-stimulating hormone. TSHR is a class A G protein-coupled receptor with a large leucine-rich extracellular domain that binds the hormone. Its complementary DNA was cloned in 1989, and receptor activation raises cyclic adenosine monophosphate (cAMP) to drive thyroid hormone synthesis and thyroid cell growth. Stimulating autoantibodies against the receptor underlie Graves' disease, so TSHR ligands are used in thyroid autoimmunity research. Small-molecule agonists were shown in 2009 to stimulate thyroid function in human thyrocytes and mice. ML-109 and MS437 act as agonists, TSHR antagonist S37a blocks receptor activation, and ML224 is an inverse agonist that lowers basal signaling.

2 Items

  • Org 274179-0
    Cat. No.
    A63967
    CAS No.
    1421683-12-6

    Org 274179-0

    Org 274179-0 is a potent allosteric antagonist of the thyroid-stimulating hormone (TSH) receptor, exhibiting an IC50 in the nanomolar range. This compound effectively inhibits TSH- and TSI-mediated activation of the TSH receptor while minimally affecting TSH potency. Org 274179-0 is valuable for research into Graves' disease (GD) and provides insights into TSH receptor modulation and related pathophysiological mechanisms.

    In stock View Details
    5 mg
    $280.00
    10 mg
    $460.00
    All 3 sizes
  • VA-K-14 hydrochloride
    Cat. No.
    A63968
    CAS No.
    1171341-19-7

    VA-K-14 hydrochloride

    VA-K-14 hydrochloride is a selective antagonist of the thyroid-stimulating hormone receptor (TSHR), exhibiting an IC50 of 12.3 μM. This compound is valuable for research applications aimed at understanding TSHR signaling pathways and its implications in thyroid-related disorders. By inhibiting TSHR activity, VA-K-14 hydrochloride aids in the exploration of potential therapeutic strategies targeting thyroid hormone regulation.

    In stock View Details
    1 mg
    $45.00
    5 mg
    $105.00
    All 6 sizes

2 Items

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