T0901317
产品说明书
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同义名 : | - |
| CAS号 : | 293754-55-9 | |
| 货号 : | A467377 | |
| 分子式 : | C17H12F9NO3S | |
| 纯度 : | 99%+ | |
| 分子量 : | 481.333 | |
| MDL号 : | MFCD03412028 | |
| 存储条件： |
Pure form Sealed in dry,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(218.14 mM)，配合低频超声助溶，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 无水乙醇: 100 mg/mL(207.76 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear PO 0.5% CMC-Na 27 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | T0901317 is a dual LXR/FXR agonist (more potent to LXR than FXR) and an inverse agonist of CAR. T0901317 at concentration ranging in 1-10μM induced FXR target genes BSEP and SHP mRNA expression in a dose-dependent manner in Huh7 cells. The transcription activity of GAL4-hCAR/LBD was repressed by T0901317 with IC50 value of 2.2μM, while the transcription activity of GAL4-LXR/LBD was increased by T0901317 with EC50 value of 0.21μM. A significant repression of Tet-induced CAR:RXR-mediated luciferase activity could also be observed after treatment with 10μM T0901317. Treatment with 10μM T0901317 for 48h reduced hCAR-mediated CYP2B6 expression on mRNA level in HepTR-hCAR cells. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| CHO cells | Function assay | Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50=16 nM | 19853462 | ||
| COS7 cells | Function assay | 16 h | Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay, EC50=11 nM | 17587573 | |
| CV1 cells | Function assay | Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay, EC50=0.14 μM | 25435151 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.39mL 2.08mL 1.04mL |
20.78mL 4.16mL 2.08mL |
| 参考文献 |
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