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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.

1 Item

  • MS437
    Cat. No.
    A63969
    CAS No.
    541535-31-3

    MS437

    MS437 is a potent stimulator of the thyroid-stimulating hormone receptor (TSHR), demonstrating an EC50 value of 13 nM. It effectively activates Gsα, Gαq, and Gα12 pathways, leading to the up-regulation of key genes such as thyroglobulin (Tg) and sodium iodine symporter (NIS). This compound is valuable for research applications focused on thyroid hormone signaling and associated disorders.

    In stock View Details
    5 mg
    $65.00
    10 mg
    $105.00
    All 5 sizes

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