生物活性

T0070907是一种有效的，选择性的PPARγ抑制剂，IC50为1 nM，比作用于PPARα和PPARδ选择性高800倍以上。T0070907是一种强有效和选择性的PPARγ抑制剂。具有明显的亲和性，IC50为1 nM。T0070907共价结合在 PPARγ 313位的半胱氨酸螺旋3上。

化学数据

分子量	277.66
分子式	C12H8ClN3O3
CAS号	313516-66-4
纯度	99.73%
溶解性（25°C）	DMSO 13 mg/mL
储存和运输条件	固体粉末： -20°C 冷藏长期储存 常温运输及临时存放

实验操作来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）

细胞实验
细胞系	Vascular endothelial cells (VECs)
方法	Cellular impedance assay VEC proliferation was assessed using a cellular impedance assay. VECs were seeded into 8-well E-plates (ACEA Biosciences, Inc., San Diego, CA, USA) at a density of 7,500 cells/well and cultured overnight. Cells were cultured with complete medium, supplemented with 0.1% dimethyl sulfoxide (DMSO) as a control, the PPARγ agonist rosiglitazone (10 μM) or the PPARγ antagonist T0070907 (15 μM) respectively, as previously described. Cellular proliferation was dynamically monitored using the iCELLigence(TM) real-time cell analysis (RTCA) system (ACEA Biosciences, Inc.) at 37°C in a 5% CO2 atmosphere for 100 h. The cell index, which reflects the adhesion, proliferation and viability of the cells through electrical impedance across interdigitated microelectrodes integrated on the bottom of the E-plates, was automatically calculated for each E-plate well using RTCA software version 1.2 (Roche Diagnostics, Basel, Switzerland) and graphs were generated in real-time using the iCELLigence(TM) system (30,31). Each treatment was performed in duplicate and three independent experiments were conducted.
浓度	15 μM
处理时间	24 h

动物实验
动物模型	Preconditioning is performed by administering a low dose (1 mg/kg) of Escherichia coli LPS (serotype 0.127:B8) intraperitoneally 24 hr before the induction of severe endotoxemia
配制	10% v/v dimethylsulfoxide [DMSO], 20–25% v/v DMSO, or saline
剂量	1 mg/kg
给药处理	intraperitoneally

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的Km系数
	动物 A的Km系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于半岛bd体育手机客户端 分子量，对于特殊半岛bd体育手机客户端 ，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	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