|2-氯-5-硝基-N-(吡啶-4-基)苯甲酰胺|CsnPharm

CAS No.: 313516-66-4

2-氯-5-硝基-N-吡啶-苯甲酰胺 Catalog No. CSN18774

Synonyms: T0070907

T0070907 is an antagonist of PPARγ with IC50 of 1 nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PPARγ

IC50:1nM
描述T0070907 is a potent and selective PPARγ antagonist with Ki value of 1nM, with >800-fold preference for PPARγ over PPARα and PPARδ with Ki values of 0.85μM and 1.8 μM. T0070907 at concentration ranging in 1nM-1μM dose-dependently antagonized the effects of rosiglitazone at concentration 1μM in HTRF assays, blocking agonist-induced recruitment of coactivator-derived peptides to PPARγ. It promoted recruitment of the transcriptional corepressor NCoR to PPARγ/RXR heterodimer^[1]. Treatment with 50μM T0070907 for 24h led loss of 70% cell adherence in trypsinized HepG2 cells, associated with reductions in phosphorylated FAK^[2].
作用机制T0070907 covalently modifies PPARγ on cysteine 313 in helix 3 of human PPARγ2. T0070907 modulates the interaction of PPARγ with cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
african green monkey OR6 cells	-	Cytotoxic assay	-	Cytotoxicity against african green monkey OR6 cells after 72 hrs by WST1 assay, CC50=2.7 μM	23891183

动物研究
剂量
Rat: 0.001 mg/kg^[3] (s.c.); 1 mg/kg^[4] (i.p.) Mice: 7.5 mg/kg^[5] (i.p.)

给药途径
s.c., i.p.
参考文献

动物研究
剂量	Rat: 0.001 mg/kg^[3] (s.c.); 1 mg/kg^[4] (i.p.) Mice: 7.5 mg/kg^[5] (i.p.)
给药途径	s.c., i.p.

[1] Lee G, Elwood F, 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.
[2] Schaefer KL, Wada K, et al. Peroxisome proliferator-activated receptor gamma inhibition prevents adhesion to the extracellular matrix and induces anoikis in hepatocellular carcinoma cells. Cancer Res. 2005 Mar 15;65(6):2251-9.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6015 mL
- 18.0074 mL
- 36.0149 mL
- 5 mM
- 0.7203 mL
- 3.6015 mL
- 7.2030 mL
- 10 mM
- 0.3601 mL
- 1.8007 mL
- 3.6015 mL

技术信息

CAS号

313516-66-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H8ClN3O3

运输

蓝冰

分子量

277.66

别名

T0070907

溶解度

DMSO	26.0 mg/mL (93.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+45% PEG 300+water

9 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

2-氯-5-硝基-N-吡啶-苯甲酰胺 Catalog No. CSN18774

靶点选择性

请登录您的专属账户

确认信息