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Km系数（3），再除以大鼠的Km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
以下数据基于产品分子量，对于特殊产品，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 |
m.cnreagent.com