1. Signaling Pathways
  2. GPCR/G Protein
  3. TSH Receptor

TSH Receptor (促甲状腺激素受体)

Thyrotropin receptor; Thyroid-stimulating hormone Receptor

The TSH receptor (TSHR) is a member of the glycoprotein hormone receptors, a subfamily of family A G protein-coupled receptors. The TSH receptor (TSHR) undergoes complex post –translational modifications including intramolecular cleavage and receptor multimerization. TSHR and its endogenous ligand thyrotropin (TSH) are of essential importance for growth and function of the thyroid gland and proper function of the TSH/TSHR system is pivotal for production and release of thyroid hormones.

The TSHR activates different G-protein subtypes and signaling pathways, whereby Gs- and Gq-induced signaling are probably of highest importance. TSH and its receptor are required for thyroid hormone synthesis and release in the thyroid gland. Dysfunctions of the TSHR are the underlying cause of various gain- or loss-of-function phenotypes associated with thyroid malfunction. It has been suggested that the TSHR is involved in the development and mechanisms of ophthalmopathy. TSHR is also a major autoantigen for autoimmune diseases of the thyroid gland. In addition, TSHR has been proposed to be a potent target against thyroid cancer with several experimental compounds under development.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12381
    ML224 Antagonist 99.71%
    ML224 (NCGC00242364) 是一种选择性的 TSHR 拮抗剂,其 IC50 值为 2.1 µM。ML224 可用于巴塞杜氏病及其他甲状腺疾病的研究。
    ML224
  • HY-114116
    ML-109 Agonist 99.12%
    ML-109 是有效的、促甲状腺激素受体 (TSHR) 的全激动剂,其 EC50 值为 40 nM。
    ML-109
  • HY-P99165
    Teprotumumab Inhibitor 99.45%
    Teprotumumab 是一种阻断 IGF-1 受体 (IGF-1R) 的人单克隆抗体。Teprotumumab 与 IGF-1R 的细胞外 α-亚基结构域配体结合。Teprotumumab 抑制纤维细胞中的 TSH 和 IGF-1 作用。Teprotumumab 可降低 TSH 依赖性 IL-6 和 IL-8 的表达和 Akt 的磷酸化。Teprotumumab 可用于甲状腺相关眼病的研究。
    Teprotumumab
  • HY-129995A
    TSHR antagonist S37a Antagonist 98.00%
    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 。
    TSHR antagonist S37a
  • HY-122974
    VA-K-14 hydrochloride Antagonist 98.20%
    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)。
    VA-K-14 hydrochloride
  • HY-114918
    MS438 Agonist
    MS438 是一种有效的促甲状腺素受体 (TSHR) 激动剂,其EC50 为 53 nM。MS438 与 TSHR 的蛇形部分结合。MS438 诱导小鼠 T4 分泌。
    MS438
  • HY-100271
    Org41841 Agonist 99.46%
    ORG41841 是促黄体激素/绒毛膜促性腺激素受体 (LHCGR) 和促甲状腺激素受体 (TSHR) 的部分激动剂,其 EC50 值分别为 0.2 和 7.7 μM。
    Org41841
  • HY-124867
    D3-βArr Modulator 99.83%
    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-Arr 1 的易位,并增强促甲状腺激素介导的体外成骨细胞分化。
    D3-βArr
  • HY-18286
    NCGC00229600 Antagonist 99.86%
    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。
    NCGC00229600
  • HY-129995
    TSHR antagonist S37b Inhibitor 99.06%
    TSHR antagonist S37b 是 TSHR antagonist S37a (HY-129995A) 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。
    TSHR antagonist S37b
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