D3-βArr
产品说明书
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同义名 : | NCGC00379308 |
| CAS号 : | 662164-09-2 | |
| 货号 : | A1155016 | |
| 分子式 : | C20H23N5 | |
| 纯度 : | 98% | |
| 分子量 : | 333.43 | |
| MDL号 : | MFCD04077665 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(359.9 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | D3-βArr is the first small molecule positive allosteric modulator of TSHR. It translocated β-arrestin 1 with EC50 value of 11.6μM, and potentiated the effect of TSH in stimulating β-Arr 1 translocation. It had no agonistic effect on cAMP production nor did it inhibit TSH-induced cAMP production in DiscoverX1 cells or primary cultures of human thyrocytes from five donors in which TSHRs are expressed at physiologic levels. D3-βArr at 10μM potentiated TSH-induced upregulation of ALPL (alkaline phosphatas) and OPN (osteopontin) mRNA levels 1.6-fold and 5.5-fold, respectively, in human U2OS-TSHR cells expressing wild-type TSHRs, which is a model of human preosteoblast-like cells, post 7 days[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.00mL 0.60mL 0.30mL |
15.00mL 3.00mL 1.50mL |
29.99mL 6.00mL 3.00mL |
| 参考文献 |
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