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维生素D相关/核受体
代谢酶 PPAR Signaling Pathway
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/ T0901317

T0901317 {[allProObj[0].p_purity_real_show]}

货号：A467377

T0901317是一种LXR和FXR选择性激动剂，EC50分别为50 nM和5 μM。

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 细胞实验

Cell Line
Concentration Treated Time Description References
HepG2 0.1 - 0.5 µM 18 hours T317 dose-dependently increased REPS2 expression and inhibited the proliferation and migration of HCC cells. Acta Pharmacol Sin. 2023 Mar;44(3):635-646.
BNLCL.2 0.1 - 0.5 µM 18 hours T317 significantly induced REPS2 protein expression in BNLCL.2 cells. Acta Pharmacol Sin. 2023 Mar;44(3):635-646.
Huh-7 0.1 - 0.5 µM 18 hours T317 significantly induced REPS2 protein expression in Huh-7 cells. Acta Pharmacol Sin. 2023 Mar;44(3):635-646.
LO2 0.1 - 0.5 µM 18 hours T317 significantly induced REPS2 protein expression in LO2 cells. Acta Pharmacol Sin. 2023 Mar;44(3):635-646.
U2OS cells 10 µM 2 days Inhibited cell proliferation, reduced KI-67 and PCNA protein levels Cell Death Dis. 2023 Jan 21;14(1):51.
HOS-MNNG cells 10 µM 2 days Inhibited cell proliferation, reduced KI-67 and PCNA protein levels Cell Death Dis. 2023 Jan 21;14(1):51.
Saos-2 cells 10 µM 2 days Inhibited cell proliferation, reduced KI-67 and PCNA protein levels Cell Death Dis. 2023 Jan 21;14(1):51.
HEK293 cells 20 nM 20 hours T0901317 induced transcriptional activity of LXR /H9251 with an EC50 of 20 nM, showing higher activity than the endogenous ligand 24,25-EC. Genes Dev. 2000 Nov 15;14(22):2831-8.
Primary human monocyte-derived macrophages 1 µM 3 hours T0901317 enhanced the expression of LXR-dependent genes including ABCA1, ABCG1, SMPDL3A, and MERTK. Cell Death Differ. 2021 Apr;28(4):1301-1316.
CD4SP thymocytes 5 µM/ml 4 hours To investigate whether LXRβ directly binds to the 5′-regulatory region of the Il7r gene and promotes its transcription Cell Mol Immunol. 2021 Aug;18(8):1969-1980.
HL-1 cardiomyocytes 10 µM 6 hours To evaluate the protective effects of T0901317 on LPS-stimulated HL-1 cardiomyocytes, the results showed that T0901317 reversed abnormal cholesterol metabolism, NLRP3 pathway, and inflammatory response. Bioeng Transl Med. 2023 Apr 6;8(3):e10517.
HCC cells 5 µM 72 hours T0901317 induced fatty acid synthase (FASN) expression in all HCC cells and antagonized TGF β-induced fibrotic marker responses in a subset of HCC cells. Oncogenesis. 2019 May 16;8(6):36.
CAFs 5 µM 74 hours T0901317 induced FASN expression in CAFs and suppressed TGF β-induced myofibroblast gene expression. Oncogenesis. 2019 May 16;8(6):36.
Hepatocytes 10 µM GF2 significantly reduced T0901317-induced fat accumulation to a similar degree as the control group J Ginseng Res. 2024 Jan;48(1):89-97.
Macrophages 10 µM GF2 reduced the expression of pro-inflammatory cytokine genes but did not affect Abca1 expression J Ginseng Res. 2024 Jan;48(1):89-97.

T0901317 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice LXRβ-deficient mice Intraperitoneal injection 0.2 mg/d per mouse 7 continuous days To investigate the effect of T0901317 on the survival of SP thymocytes in LXRβ-deficient mice, the results showed that T0901317 promoted the survival of SP thymocytes in the presence of LXRβ, but had no significant effect in LXRβ-deficient mice Cell Mol Immunol. 2021 Aug;18(8):1969-1980.
BALB/c Nude mice Subcutaneous tumour model Subcutaneous injection 1 μg Every 3 days, until the end of the experiment Inhibited tumour growth, significantly reduced tumour volume and weight Cell Death Dis. 2023 Jan 21;14(1):51.
C57BL/6 or Balbc mice Cecal ligation and puncture (CLP) model Intraperitoneal injection 10 mg/kg Single administration To evaluate the protective effects of T0901317 on CLP model mice, the results showed that T0901317 significantly reduced sepsis score and improved cardiac dysfunction. Bioeng Transl Med. 2023 Apr 6;8(3):e10517.
Mice and hamsters C57BL/6 mice and Golden Syrian hamsters Oral 5 mg/kg Once daily for 7 days T0901317 significantly increased plasma triglyceride and phospholipid levels in mice and hamsters by activating LXR, and induced the expression of genes associated with fatty acid biosynthesis. Genes Dev. 2000 Nov 15;14(22):2831-8.
C57BL/6 mice Wild-type mice Intraperitoneal injection 5 mg/kg Once daily for 10 days T317 significantly increased REPS2 protein and mRNA levels in the liver of mice. Acta Pharmacol Sin. 2023 Mar;44(3):635-646.
Mice High-fat diet-induced MASLD model Oral 50 mg/kg Once daily for 6 weeks GF2 ameliorated high-fat diet-induced MASLD, reducing hepatic fat accumulation and inflammatory response J Ginseng Res. 2024 Jan;48(1):89-97.

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 481.33
SMILES Code O=S(C1=CC=CC=C1)(N(CC(F)(F)F)C2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)=O
MDL No. MFCD03412028
别名
运输蓝冰
InChI Key SGIWFELWJPNFDH-UHFFFAOYSA-N
Pubchem ID 447912
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四
方案 五

Tags: T0901317 | 293754-55-9 | T 0901317 | T-0901317 | LXR Agonist | Vitamin D Related/Nuclear Receptor | Metabolic Enzyme/Protease | Apoptosis | LXR | FXR | ROR | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | T0901317 纯度/质量文件 | T0901317 生物活性 | T0901317 动物研究 | T0901317 参考文献 | T0901317 实验方案 | T0901317 技术信息

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