|N-(4-(1,1,1,3,3,3-六氟-2-羟基丙-2-基)苯基)-N-(2,2,2-三氟乙基)苯磺酰胺|CsnPharm

CAS No.: 293754-55-9

T0901317 Catalog No. CSN15954

Synonyms: T-1317;TO-91317;TO 901317

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

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靶点选择性

生物活性

实验方案

技术信息

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
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.)

给药途径
p.o.
参考文献

动物研究
剂量	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.)
给药途径	p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0776 mL
- 10.3878 mL
- 20.7757 mL
- 5 mM
- 0.4155 mL
- 2.0776 mL
- 4.1551 mL
- 10 mM
- 0.2078 mL
- 1.0388 mL
- 2.0776 mL

技术信息

CAS号

293754-55-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12F9NO3S

运输

蓝冰

分子量

481.33

别名

T-1317;TO-91317;TO 901317;TO-091317

溶解度

DMSO	500.0 mg/mL (1038.8 mM) warming
Water	insoluble

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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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
HepG2 cells	-	Function assay	-	Effect on SREBP1c gene expression in human HepG2 cells, EC50=0.061 μM	18973288
HuH7 cells	-	Function assay	-	Upregulation of SREB1c mRNA level in human HuH7 cells, EC50=0.036 μM	20382019
human H4 cells	-	Function assay	-	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay, EC50=3.6 μM	17723298
mouse J774 cells	-	Function assay	-	Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression, EC50=0.027 μM	19853462
mouse J774A1 cells	-	Function assay	18 h	Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR, EC50=0,034 μM	19394832
SH-SY5Y cells	-	Function assay	24 h	Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50=0.075 μM	19264481
THP1 cells	-	Function assay	-	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL, EC50=3 nM	19962892

T0901317 Catalog No. CSN15954

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