| CAS NO: | 610318-54-2 |
RGX-104, also known as SB 742881, is a liver X receptor beta (LXR) agonist with potential immunomodulating and antineoplastic activities. RGX-104 modulates innate immunity via transcriptional activation of the ApoE gene.
Oral administration of RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells.
| 分子量 | 596.08 |
| 分子式 | C34H33ClF3NO3 |
| CAS号 | 610318-54-2 |
| 纯度 | >99.5% |
| 溶解性（25°C） | DMSO 90 mg/mL |
| 储存和运输条件 | 2-8°C, protect from light, sealed 常温运输及临时存放 |
| 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。
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 | 1.6776 mL | 8.3881 mL | 16.7763 mL |
| 5 mM | 0.3355 mL | 1.6776 mL | 3.3553 mL |
| 10 mM | 0.1678 mL | 0.8388 mL | 1.6776 mL |
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