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。
| 生物活性 | T0901317 is an orally active and highly selectiveLXRagonist with anEC50of 20 nM for LXRα[1]. T0901317 activatesFXRwith anEC50of 5 μM[2]. T0901317 isRORαandRORγdual inverse agonist withKivalues of 132 nM and 51 nM, respectively[3]. T0901317 inducesapoptosisand inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice[4][5]. |
| IC50& Target | EC50: 20 nM (LXRα) and 5 μM (FXR)[1][2]
Ki: 132 nM (RORα) and 51 nM (RORγ)[3] |
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[5].
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[5].
T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis[5].
T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours[5].
Cell Proliferation Assay[5] | 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[5] | 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[5] | 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[5] | 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. |
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体内研究
(In Vivo) | T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis[5].
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[6].
| Animal Model: | 8- to 10-week-old LDL receptor null mice[5] | | Dosage: | 10 mg/kg | | Administration: | Orally; daily; for 12 weeks | | Result: | Inhibited the progression of atherosclerosis. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(207.76 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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-CDin saline) Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution *以上所有助溶剂都可在本网站选购。
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