T0901317|293754-55-9|293754-55-9-陌孚医药/Medlife

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T0901317 293754-55-9

目录号: PC14744 纯度: ≥98%

CAS No. :293754-55-9

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PC14744-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥588.00	请登录

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中文名称

T0901317

中文别名

N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺;N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]-苯磺酰胺

英文名称

T0901317

英文别名

Benzenesulfonamide,N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-;T0901317;N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide;T-0901317;T 1317;TO 901317;N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide;T 0901317;TO901317;A07663A39I;Benzenesulfonamide, N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-;N-(2,2,2-TRIFLUOROETHYL)-N-{4-[2,2,2-TRIFLUORO-1-HYDROXY-1-(TRIFLUOROMETHY

Cas No.

293754-55-9

分子式

C₁₇H₁₂F₉NO₃S

分子量

481.33

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

性状

Solid

IC50 & Target[1][2]

EC50: 20 nM (LXRα) and 5 μM (FXR)
Ki: 132 nM (RORα) and 51 nM (RORγ)

体外研究(In Vitro)

T0901317 (5-50 μM; 72 hours) significantly inhibits cellular proliferation in CaOV3, SKOV3, A2780 (human ovarian carcinoma cell lines) in a dose-dependent and time-dependent manner.
T0901317 (10 μM; 24-72 hours) decreases the percentage of cells in S phase and increases the percentage of cells in the G0/G1 phase, indicating a cell cycle arrest at the G1-S checkpoint. The percentage of cells in G0/G1 phase increases in a time-dependent manner.
T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis.
T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	A2780, CaOV3 and SKOV3 ovarian cancer cell lines
Concentration:	5, 10, 20, 40 or 50 μM
Incubation Time:	72 hours
Result:	Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner.

Cell Cycle Analysis

Cell Line:	A2780, CaOV3 and SKOV3 cells
Concentration:	10 μM
Incubation Time:	24, 48 or 72 hours
Result:	Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase.

Apoptosis Analysis

Cell Line:	CaOV3 cells
Concentration:	10 to 40 μM
Incubation Time:	24 hours
Result:	Resulted in a significant increase of cells in early apoptosis.

Western Blot Analysis

Cell Line:	CaOV3 cells
Concentration:	5 to 40 μM
Incubation Time:	48 hours
Result:	Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.

体内研究(In Vivo)

T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis.
T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8- to 10-week-old LDL receptor null mice
Dosage:	10 mg/kg
Administration:	Orally; daily; for 12 weeks
Result:	Inhibited the progression of atherosclerosis.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8. [Information]

[2]. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7. [Information]

[3]. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol P [Information]

[4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13. [Information]

[5]. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. [Information]

[6]. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (207.76 mM; Need ultrasonic)

Ethanol : 100 mg/mL (207.76 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0776 mL	10.3879 mL	20.7758 mL
5 mM	0.4155 mL	2.0776 mL	4.1552 mL
10 mM	0.2078 mL	1.0388 mL	2.0776 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.5 mg/mL (5.19 mM); Suspended solution; Need ultrasonic
5.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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