生物活性
TUG-424 is expected to be useful in the exploration of FFA1 and may also be valuable as a lead structure for new potential antidiabetic therapeutics. TUG-424 significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity. It enhanced glucose-stimulated insulin secretion in a rat beta-cell line already at 100 nM and from isolated mouse islets through FFA1.
GPR40 (now FFA1) was formerly an orphan GPCR whose endogenous ligands have recently been identified as free fatty acids (FFAs). The receptor appears to be involved in the pathophysiology of type 2 diabetes and is a drug target because of its role in FFA-mediated enhancement of glucose-stimulated insulin release.
化学数据
| 分子量 | 264.32 |
| 分子式 | C18H16O2 |
| CAS号 | 1082058-99-8 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO: ≥10 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 | 3.7833 mL | 18.9165 mL | 37.8329 mL |
| 5 mM | 0.7567 mL | 3.7833 mL | 7.5666 mL |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7833 mL |
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