T0070907
目录号 : GC12820
A potent and selective PPARγ antagonist
Cas No.:313516-66-4
Sample solution is provided at 25 µL, 10mM.
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T0070907 is a selective antagonist of peroxisome proliferator-activated receptor γ (PPARγ) with IC50 value of 1nM [1].
T0070907 shows high affinity to PPARγ with Ki of 1nM. The Ki values of it to PPARα and PPARδ are 0.85 and 1.8μM, respectively, demonstrating the high selectivity of T0070907. It is found that T0070907 binds PPARγ within the cysteine 313 in helix 3 of human PPARγ2, subsequently blocks PPARγ function. In transient transfection assay, T0070907 inhibits the transactivation of PPARγ in the presence of rosiglitazone (a PPARγ agonist) with IC50 value in the nM range. T0070907 can block the induction of adipogenesis of the adipogenic cell line 3T3-L1. Additionally, T0070907 is found to suppress the interaction between PPARγ and the coactivator derived peptide, while promoting the recruitment of the NCoR-derived peptide to PPARγ. Furthermore, T0070907 can also promote a significant increase in the recruitment of NCoR to the PPARγ/RXRα heterodimer [1].
References:
[1] Lee G, Elwood F, McNally J, Weiszmann J, Lindstrom M, Amaral K, Nakamura M, Miao S, Cao P, Learned RM, Chen JL, Li Y. 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.
| Cell experiment [1]: | |
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Cell lines |
HeLa, SiHa, and Me180 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >13.9 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
50 μM |
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Applications |
Three cervical cancer cell lines (HeLa, SiHa, and Me180) were treated with a PPARγ inhibitor, T0070907, and/or radiation. T0070907 has significantly decreased the tubulin levels in a time-dependent manner in ME180 cells. The decrease in the tubulin levels after T0070907 in ME180 and SiHa cells was associated with significant increase in the cells at the G2/M phase. The changes in the tubulin and G2/M phase were not evident in HeLa cells. T0070907 reduced the protein levels of PPARγ; however, PPARγ silencing had no effect on the α-tubulin level in ME180 cells suggesting the PPARγ-dependent and -independent actions of T0070907. |
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References: [1] 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. | |
| Cas No. | 313516-66-4 | SDF | |
| 化学名 | 2-chloro-5-nitro-N-pyridin-4-ylbenzamide | ||
| Canonical SMILES | C1=CC(=C(C=C1[N+](=O)[O-])C(=O)NC2=CC=NC=C2)Cl | ||
| 分子式 | C12H8ClN3O3 | 分子量 | 277.66 |
| 溶解度 | ≥ 27.8 mg/mL in DMSO, ≥ 4.77 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6015 mL | 18.0076 mL | 36.0153 mL |
| 5 mM | 0.7203 mL | 3.6015 mL | 7.2031 mL |
| 10 mM | 0.3602 mL | 1.8008 mL | 3.6015 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet