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T0901317 {[allProObj[0].p_purity_real_show]}

货号:A467377

T0901317 is a selective agonist for LXR and FXR with EC50 of 50 nM and 5 μM, respectively.

T0901317 化学结构 CAS号:293754-55-9
T0901317 化学结构
CAS号:293754-55-9
T0901317 3D分子结构
CAS号:293754-55-9
T0901317 化学结构 CAS号:293754-55-9
T0901317 3D分子结构 CAS号:293754-55-9
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T0901317 纯度/质量文件 产品仅供科研

货号:A467377 标准纯度: {[allProObj[0].p_purity_real_show]}
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T0901317 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.

T0901317 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
HEK293 cells Function assay Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation, EC50=19 nM 20350005

T0901317 动物研究

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.

T0901317 参考文献

[1]Repa JJ, Turley SD, et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science. 2000 Sep 1;289(5484):1524-9.

[2]Houck KA, Borchert KM, et al. T0901317 is a dual LXR/FXR agonist. Mol Genet Metab. 2004 Sep-Oct;83(1-2):184-7.

[3]Kanno Y, Tanuma N, et al. TO901317, a potent LXR agonist, is an inverse agonist of CAR. J Toxicol Sci. 2013;38(3):309-15.

T0901317 实验方案

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

T0901317 技术信息

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

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