TSHR antagonist S37a |
| رقم الكتالوجGC62519 |
مضاد TSHR S37a هو مضاد انتقائي للغاية لمستقبلات الثيروتروبين (TSHR) ، مع إمكانية علاج اعتلال حجرة جريفز
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2143452-20-2
Sample solution is provided at 25 µL, 10mM.
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TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves’ orbitopathy[1].
TSHR antagonist S37a exhibits inhibition activity for TSHR, with IC50s of 40 µM and approximately 20 µM for mTSHR and hTSHR, respectively, in HEK293 cells[1].TSHR antagonist S37a not only inhibits the TSHR activation by thyrotropin itself but also activation by monoclonal TSAb M22 (human), KSAb1 (murine), and the allosteric small-molecule agonist C2[1].
TSHR antagonist S37a also inhibits cyclic adenosine monophosphate formation by oligoclonal TSAb, which are highly enriched in GO patients’ sera[1].TSHR antagonist S37a (10 mg/kg ;i.g.) displays no toxicity and a remarkable 53% oral bioavailability in mice[1].
[1]. Marcinkowski P, et al. A New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves’ Orbitopathy. Thyroid. 2019 Jan;29(1):111-123.
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