T0901317 is a selective agonist for LXR and FXR with EC50 of 50 nM and 5 μM, respectively.
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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 | ||
HEK293 cells | Function assay | Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation, EC50=19 nM | 20350005 | ||
Dose | Cynomolgus monkey: 10 mg/kg[4] (p.o.) Rat: 10 mg/kg[5] (p.o.) BALB/c mice: 10 mg/kg - 100 mg/kg[6] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.39mL 2.08mL 1.04mL |
20.78mL 4.16mL 2.08mL |
CAS号 | 293754-55-9 |
分子式 | C17H12F9NO3S |
分子量 | 481.333 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
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 |
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 |