TSHR antagonist S37a|2143452-20-2|-陌孚医药/Medlife

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TSHR antagonist S37a

目录号: PL12487 纯度: ≥98%

CAS No. :2143452-20-2

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中文名称	TSHR antagonist S37a
中文别名	化合物 T13217
英文名称	TSHR antagonist S37a
英文别名	TSHR antagonist S37a;CID 156588665;5,9-Methanothiazolo[5',4':5,6]thiopyrano[2,3-f]isoindole-2,6,8(7H)-trione, 3,4a,5,5a,8a,9,9a,10-octahydro-7,10-diphenyl-, (4aS,5S,5aR,8aR,9R,9aS,10R)-;TSHR antagonist S37a,TSHR antagonist S-37a
Cas No.	2143452-20-2
分子式	C₂₅H₁₉N₂O₃S₂
分子量	459.56
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves orbitopathy.
性状	Solid
IC50 & Target[1][2]	TSHR
体外研究(In Vitro)	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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	TSHR antagonist S37a also inhibits cyclic adenosine monophosphate formation by oligoclonal TSAb, which are highly enriched in GO patients sera. TSHR antagonist S37a (10 mg/kg ;i.g.) displays no toxicity and a remarkable 53% oral bioavailability in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (217.12 mM; Need ultrasonic)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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