生物活性
SB290157 is a selective antagonist of complement anaphylatoxin C3a receptor, a 74 amino acid proinflammatory peptide that is a potent chemotaxin for eosinophils, macrophages and mast cells, and has recently been found to be involved in nonimmunological roles in osteoblast differentiation, angiogenesis, and lipid metabolism. SB290157 is selective for C3aR over C5aR or other chemotactic GPCRs with an IC50 of 200 nM. It effectively blocks C3aR in humans, rat, guinea pig, and mouse.SB290157 was found to inhibit diet-induced obesity, metabolic dysfunction, and adipocyte signaling, in addition to inhibiting macrophage signaling.
化学数据
| 分子量 | 526.51 |
| 分子式 | C22H28N4O4.CF3CO2H |
| CAS号 | 1140525-25-2 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO ≥ 90 mg/mL
Ethanol ≥ 60 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 | 1.8993 mL | 9.4965 mL | 18.993 mL |
| 5 mM | 0.3799 mL | 1.8993 mL | 3.7986 mL |
| 10 mM | 0.1899 mL | 0.9496 mL | 1.8993 mL |
