T0901317
目录号 : KM2684 CAS No. : 293754-55-9 纯度 : 98%

T0901317 是口服有效且高度选择性的 LXR 激动剂,对 LXRα 的 EC50 为 20 nM。T0901317 激活 FXR,EC50 为 5 μM。T0901317 是 RORα 和 RORγ 双重反向激动剂,Ki 值分别为 132 nM 和 51 nM。T0901317 诱导细胞凋亡 (apoptosis),并抑制低密度脂蛋白 (LDL) 受体缺失小鼠动脉粥样硬化的发展。

规格 价格 是否有货 数量
10mg
In-stock
50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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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 Ki 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.

体外研究

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.

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

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.

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.
分子式
C17H12F9NO3S
分子量
481.33
CAS号
293754-55-9
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: 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。

  • 2.

    请依序添加每种溶剂: 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。

  • 3.

    请依序添加每种溶剂: 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.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.5 mg/mL (5.19 mM); Suspended solution; Need ultrasonic

  • 5.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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