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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-PPAR-T0070907
T0070907

Chemical Structure : T0070907

CAS No.: 313516-66-4

T0070907 (T-0070907;T 0070907)

货号: PC-43387Not For Human Use, Lab Use Only.

T0070907 is a potent, selective, covalent PPARγ antagonist with binding IC50 of 1 nM, >800-fold preference for PPARγ over PPARα and PPARδ.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

T0070907 is a potent, selective, covalent PPARγ antagonist with binding IC50 of 1 nM, >800-fold preference for PPARγ over PPARα and PPARδ.
T0070907 specifically blocks PPARγ function in both cell-based reporter gene and adipocyte differentiation assays, with no effect on FXR, LXR, PR.
T0070907 modulates the interaction of PPARγ with cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain (LBD).
T0070907 significantly more efficient at causing cancer cell death than the activators troglitazone and rosiglitazone.

物理化学性质&存储条件

分子量 277.6632
分子式 C12H8ClN3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-

参考文献

1. Lee G, et al. J Biol Chem. 2002 May 31;277(22):19649-57.

2. Schaefer KL, et al. Cancer Res. 2005 Mar 15;65(6):2251-9.

3. Masuda T, et al. Clin Cancer Res. 2005 Jun 1;11(11):4012-21.

4. Zaytseva YY et al. Anticancer Res. 2011, 31(3), 813-823.

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