产品说明书
SR3335
 |
同义名 : | - |
| CAS号 : | 293753-05-6 | |
| 货号 : | A129464 | |
| 分子式 : | C13H9F6NO3S2 | |
| 纯度 : | 98% | |
| 分子量 : | 405.336 | |
| MDL号 : | MFCD02724814 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(259.04 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The RORs have been characterized as constitutively active receptors displaying the ability to activate transcription in the absence of a ligand. The retinoic acid receptor-related orphan receptor α (RORα) is an orphan receptor that has been demonstrated to play an important role in regulation of metabolism [3]. SR3335 is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM [3]. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR3335 significantly inhibits the constitutive transactivation activity of RORα (IC50=480 nM)(partial inverse agonist activity), but has no effect on the activity of LXRα and RORγ [3]. Pharmacokinetic studies indicate that SR3335 displays reasonable exposure following an i.p. injection into mice. The ability of SR3335 is assessed to suppress gluconeogenesis using a diet induced obesity (DIO) mouse model where the mice where treated with 15 mg/kg b.i.d., i.p. for 6-days followed by a pyruvate tolerance test. SR3335 treated mice displays lower plasma glucose levels following the pyruvate challenge consistent with suppression of gluconeogenesis. Importantly, mice treated with SR3335 displayed no difference in body weight or food intake after 7-days of treatment with SR3335 [3]. | ||
| 作用机制 | SR3335 is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.34mL 2.47mL 1.23mL |
24.67mL 4.93mL 2.47mL |
| 参考文献 |
|---|