生物活性
SR9238 induces increased interaction of CoRNR box peptides derived from NCoR (NCoR ID1 and NCoR ID2) with both LXRα and LXRβ, while causing decreased interaction with a coactivator NR box peptide derived from TRAP220. SR9238-induced recruitment of CoRNR box peptides is dose-dependent for both LXRα and LXRβ. HepG2 cells treated with SR9238 result in a significant decrease in Fasn and Srebp1c mRNA expression.
SR9238-treated mice display greatly reduced lipid content in the liver. SR9238-treated DIO mice display considerably lower intensity of F4/80 staining versus vehicle-treated DIO mice consistent with a beneficial effect of SR9238 on non-alcoholic steatohepatitis.
化学数据
分子量 | 595.73 |
分子式 | C31H33NO7S2 |
CAS号 | 1416153-62-2 |
纯度 | 100.00% |
溶解性(25°C) | DMSO ≥ 25 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 |
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 | 1.6786 mL | 8.3931 mL | 16.7861 mL |
5 mM | 0.3357 mL | 1.6786 mL | 3.3572 mL |
10 mM | 0.1679 mL | 0.8393 mL | 1.6786 mL |