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TSH Receptor(促甲状腺激素受体)

The thyrotropin receptor (TSHR), one of the primary antigens in autoimmune thyroid disease, is a target of both antigen-specific T cells and antibodies in patients with this condition. Autoantibodies to the TSHR (TSHR-Ab) act as thyroid stimulating factor (TSH) agonists in autoimmune hyperthyroidism (Robert Graves disease) but as TSH antagonists in autoimmune hypothyroidism (Hashimoto thyroiditis). The TSHR antigen is primarily expressed in the epithelial cells of the thyroid follicles, but TSHR mRNA and protein have been reported in a variety of cell types, some of which show evidence of receptor activity.

TSH receptor (TSHR) plays an important role in the pathogenesis of thyroid disease, a TSHR antagonist could be a novel treatment.

TSH, acting through the TSH receptor, is the major stimulator of thyroid cell growth, differentiation and function.

  1. Cat.No. 产品名称 Information
  2. GC65946 VA-K-14 hydrochloride VA-K-14 hydrochloride 是一种特异性促甲状腺激素受体 (TSHR) 拮抗剂 (IC50= 12.3 μM)。
  3. GC64079 NCGC00229600 NCGC00229600 是 TSHR 的变构反向激动剂。NCGC00229600 抑制 TSH 和刺激在 Graves 病中内源表达的 TSHRs 的抗体激活。
  4. GC62519 TSHR antagonist S37a TSHR antagonist S37a 是一个高选择性的促甲状腺激素受体 TSHR 拮抗剂,具有研究格雷夫斯眼窝病的潜力 。
  5. GC62506 TSHR antagonist S37b TSHR antagonist S37b 是 TSHR antagonist S37a 的低活性异构体,对促甲状腺激素受体 TSHR 有较小的抑制作用。TSHR antagonist S37b 可以用于甲状腺功能的研究。
  6. GC60737 D3-βArr D3-βArr是一种促甲状腺激素受体正变构调节剂,通过促甲状腺激素受体直接激活启动β-Arr1的易位,并增强促甲状腺激素介导的体外成骨细胞分化。
  7. GC19543 NCGC00379308 NCGC00379308 是促甲状腺激素受体 (TSHR) 的正变构调节剂,它通过直接激活 TSHR 启动 β-Arr 1 的易位,并在体外增强 TSH 介导的前成骨细胞分化。
  8. GC32423 Org41841 A dual LH and TSH receptor agonist
  9. GC31490 ML-109 ML-109是有效的、促甲状腺激素受体(TSHR)的全激动剂,其EC50值为40nM。
  10. GC12956 ML224 ML224(NCGC00242364; ANTAG3) 是一种选择性 TSHR 反向激动剂;抑制 TSH 刺激的 cAMP 产生,IC50 = 2.3 μM。

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