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TSHR antagonist S37a
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TSHR antagonist S37a图片
CAS NO:2143452-20-2
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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 。
Cas No.2143452-20-2
分子式C25H20N2O3S2
分子量460.57
溶解度DMSO : 100 mg/mL (217.12 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.