產(chǎn)品屬性：
產(chǎn)品名稱 | TSHR antagonist S37a |
規(guī)格 | 10mM*1 mL in DMSO、5 mg、10 mg、25 mg、50 mg、100 mg |
貨號(hào) | EY-01Y15483 |
Cas No.: 2143452-20-2
別名: N/A
化學(xué)名: N/A
分子式: C25H20N2O3S2
分子量: 460.57
溶解度: DMSO : 100 mg/mL (217.12 mM; Need ultrasonic)
儲(chǔ)存條件: 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
產(chǎn)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.
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