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T0070907

T0070907用途

T0070907 是有效的 PPARγ 拮抗剂，潜在的 RAD51 抑制剂，能够抑制 PPARγ 的活性，K_i 值为 1 nM。

T0070907名称

[ CAS 号 ]:
313516-66-4

[ 中文名 ]:
2-氯-5-硝基-N-4-吡啶基苯甲酰胺

[ 英文名 ]:
T0070907

[英文别名 ]:

Benzamide,2-chloro-5-nitro-N-4-pyridinyl
2-chloro-5-nitro-N-pyridin-4-yl-benzamide
Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-
2-Chloro-5-nitro-N-(4-pyridinyl)benzamide
2-Chloro-5-nitro-N-4-pyridinylbenzamide
2-chloro-5-nitro-N-(pyridin-4-yl)benzamide
T0070907

T0070907生物活性

[ 描述 ]:

T0070907是有效的 PPARγ 拮抗剂,Ki值为1 nM。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> PPAR

信号通路 >> 细胞周期/DNA损伤 >> RAD51

研究领域 >> 癌症

[ 靶点 ]

PPARγ:1 nM (Ki)

PPARδ:1.8 μM (Ki)

PPARα:0.85 μM (Ki)

[体外研究]

T0070907(50μM)预处理损害了用辐射(4Gy)处理的ME-180和SiHa细胞中IR诱导的DNA DSB的修复。 T0070907(0-50μM)显着降低ME-180和SiHa细胞中DNA-PKcs和RAD51蛋白的水平[1]。 T0070907(50μM)处理以时间依赖性方式降低α-和β-微管蛋白的水平,减少DNA的合成,并防止辐射诱导的ME180和SiHa细胞的细胞周期调节蛋白的改变[2] ]。 T0070907(10μM)具有脂肪细胞特异性和PPARγ非依赖性细胞毒性。 T0070907增加未成熟脂肪细胞的氧化应激[3]。 T0070907(1μM)通过脂肪形成细胞系3T3-L1的各种处理阻断脂肪生成的诱导。 T0070907共价修饰人PPAR 2螺旋3中半胱氨酸313上的PPAR [4]。

[激酶实验]

为了确定T0070907与PPAR的结合亲和力，用以下修饰进行闪烁亲近测定（SPA）。 90μL反应物含有SPA缓冲液（10mM K2HPO4,10mM KH2PO4,2mM EDTA，50mM NaCl，1mM二硫苏糖醇，2mM CHAPS，10％（v / v）甘油，pH7.1），50ng GST- PPAR（或150ng GST-PPAR），5nM 3H标记的放射性配体和5μL的Me 2 SO中的T0070907。在室温下温育1小时后，加入10μL涂有聚赖氨酸的SPA珠（在SPA缓冲液中20mg / mL），将混合物温育1小时，然后在Packard Topcount中读数。 [3H]罗格列酮用于PPAR，[3H] GW2433用于PPAR和PPAR。

[参考文献]

[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

[相关活性小分子]

T0070907物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
381.7±37.0 °C at 760 mmHg

[ 分子式 ]:
C₁₂H₈ClN₃O₃

[ 分子量 ]:
277.663

[ 闪点 ]:
184.6±26.5 °C

[ 精确质量 ]:
277.025421

[ PSA ]:
87.81000

[ LogP ]:
2.25

[ 外观性状 ]:
white

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.684

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
DMSO: >10mg/mL | Soluble in DMSO at 10mg/ml. Insoluble in water.

T0070907MSDS

详细MSDS(安全技术说明书)

T0070907安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H319

[ 警示性声明 ]:
P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-36

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933399090

T0070907合成路线

详细合成路线

T0070907上下游产品

T0070907上游产品

T0070907下游产品

T0070907海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

T0070907文献

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Environ. Res. 140 , 145-56, (2015)

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Bioenergetic programming of macrophages by the apolipoprotein A-I mimetic peptide 4F.

Biochem. J. 467(3) , 517-27, (2015)

The apoA-I (apolipoprotein A-I) mimetic peptide 4F favours the differentiation of human monocytes to an alternatively activated M2 phenotype. The goal of the present study was to test whether the 4F-m...

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