T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα^[1]. T0901317 activates FXR with an EC₅₀ of 5 μM^[2]. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively^[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice^[4][5].

EC50: 20 nM (LXRα) and 5 μM (FXR)^[1][2]
Ki: 132 nM (RORα) and 51 nM (RORγ)^[3]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

481.33

C₁₇H₁₂F₉NO₃S

293754-55-9

Room temperature in continental US; may vary elsewhere.

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

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。

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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 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。

  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.

  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

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

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

  [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 Pharmacol. 2010 Feb;77(2):228-36.

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

  [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.

  [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.