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.

3 Items

  • TSHR antagonist S37a
    Cat. No.
    A63965

    TSHR antagonist S37a

    TSHR Antagonist S37a is a selective inhibitor of the thyrotropin receptor (TSHR), demonstrating significant potential for therapeutic applications in Graves' orbitopathy. This compound effectively modulates TSHR signaling, thereby influencing thyroid hormone activity and offering insights into the pathophysiology of thyroid-related disorders. Its specificity and efficacy make it a valuable tool for research in endocrine and autoimmune disease studies.

    1 mg
    $120.00
    5 mg
    $310.00
    All 6 sizes
  • Benzylthiouracil
    Cat. No.
    A63970

    Benzylthiouracil

    Synonyms: 6-Benzyl-2-thiouracil

    Benzylthiouracil is a potent inhibitor of the TSH receptor, employed primarily in the management of hyperthyroidism. By blocking the effects of thyroid-stimulating hormone, it reduces the production of thyroid hormones, thereby alleviating symptoms associated with hyperthyroidism. This compound is valuable in both clinical settings and research applications focused on thyroid function and related disorders.

    25 mg
    $35.00
    50 mg
    $50.00
    All 5 sizes
  • TSHR antagonist S37b
    Cat. No.
    A63972

    TSHR antagonist S37b

    TSHR antagonist S37b is an enantiomeric compound that functions as a thyrotropin receptor (TSHR) inhibitor, exhibiting reduced efficacy compared to its counterpart, S37a. While S37b demonstrates a limited impact on TSHR inhibition, it serves as a valuable tool for investigations into thyroid function and dysregulation. This compound is suitable for research focused on the role of TSHR in thyroid-related conditions.

    5 mg
    $330.00
    10 mg
    $540.00
    All 5 sizes

3 Items

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