生物活性
WWL229 is a highly selective inhibitor of mouse Carboxylesterase 3 (Ces3) and human CES1 (orthologue of mCes3), serine hydrolases involved in lipolysis in addition to their activities as liver detoxification enzymes. WWL229 inhibits mCes3 with an IC50of 10 μM, but not Ces1f, ABHD6 or other tested serine hydrolases. In a recent study, hCES1 activity was found to be increased two-fold in obese individuals and patients with type 2 diabetes compared to lean subjects, and is thought to generate surplus fatty acids that can deposit ectopically in tissues. WWL229 inhibits adipocyte basal lipolysis and promotes differentiation and lipid storage in adipocytes.
化学数据
| 分子量 |
322.36 |
| 分子式 |
C16H22N2O5 |
| CAS号 |
1338575-28-2 |
| 纯度 |
>98% |
| 溶解性（25°C） |
|
| 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
以下数据基于半岛bd体育手机客户端 分子量，对于特殊半岛bd体育手机客户端 ，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 |
3.1021 mL |
15.5106 mL |
31.0212 mL |
| 5 mM |
0.6204 mL |
3.1021 mL |
6.2042 mL |
| 10 mM |
0.3102 mL |
1.5511 mL |
3.1021 mL |
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