T0070907 is a potent PPARγ antagonist with a K_i of 1 nM.

T0070907 (50 μM) pre-treatment impairs repair of IR-induced DNA DSBs in both ME-180 and SiHa cells treated with irradiated (4 Gy). T0070907 (0-50 μM) significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells^[1]. T0070907 (50 μM) treatment reduces the levels of α- and β-tubulin protein in a time-dependent manner, decreases the synthesis of DNA, and prevents the radiation-induced alterations in the cell cycle regulatory proteins of ME180 and SiHa cells^[2]. T0070907 (10 µM) has cytotoxicity in an adipocyte-specific and PPARγ-independent manner. T0070907 increases oxidative stress in immature adipocytes^[3]. T0070907 (1 μM) blocks the induction of adipogenesis by various treatments of the adipogenic cell line 3T3-L1. T0070907 covalently modifies PPAR on cysteine 313 in helix 3 of human PPAR 2^[4].

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.

277.66

C₁₂H₈ClN₃O₃

313516-66-4

Room temperature in continental US; may vary elsewhere.

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

In Vitro: 

DMSO : 62.5 mg/mL (225.10 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (insoluble)

*

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: ≥ 1 mg/mL (3.60 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (3.60 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (3.60 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (3.60 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (3.60 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (3.60 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 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. An Z, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51. Toxicol In Vitro. 2016 Dec;37:1-8

  [2]. An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

  [3]. Kawahara A, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34

  [4]. Lee G, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4

To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90 μL reaction contains SPA buffer (10 mM K₂HPO₄, 10 mM KH₂PO₄, 2 mM EDTA, 50 mM NaCl, 1 mM dithiothreitol, 2 mM CHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPAR (or 150 ng of GST-PPAR), 5 nM ³H-labeled radioligands, and 5 μL of T0070907 in Me₂SO. After incubation for 1 h at room temperature, 10 μL of polylysine-coated SPA beads (at 20 mg/mL in SPA buffer) are added, and the mixture is incubated for 1 h before reading in Packard Topcount. [³H]Rosiglitazone is used for PPAR, and [³H]GW2433 is used for PPAR and PPAR.

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.

• [1]. An Z, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51. Toxicol In Vitro. 2016 Dec;37:1-8

  [2]. An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

  [3]. Kawahara A, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34

  [4]. Lee G, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4