产品
编 号：F273057
分子式：C25H20N2O3S2
分子量：460.57
分子式：C25H20N2O3S2
分子量：460.57
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 2143452-20-2
产品详情
生物活性：
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
体内研究：
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.Animal Model:SWISS (CD1) mice (38-43 g)
Dosage:10 mg/kg
Administration:Oral gavage
Result:Displays a remarkable 53% oral bioavailability as well asa half‐life of 2.9 hours after oral application.
体外研究：
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.
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
体内研究：
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.Animal Model:SWISS (CD1) mice (38-43 g)
Dosage:10 mg/kg
Administration:Oral gavage
Result:Displays a remarkable 53% oral bioavailability as well asa half‐life of 2.9 hours after oral application.
体外研究：
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.
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