生物活性
WWL70 is a selective inhibitor of α/β-hydrolase domain-containing 6 (ABHD6), a serine hydrolase that acts as an alternative hydrolase of the endocannabinoid 2-arachidonoylglycerol (2-AG). It has an IC50 value of 55-70 nM and 90-95% inihibition of ABDH6. WWL70 hs been used in a variety of studies as an ABHD6 antagonist. It was shown to rescue impaired function of mGluR5 signaling, resulting in pain inhibition in arthritic rats. WWL70 was also used to show that ABHD6 is involved in brown adipose function and white adipose browning, and is a potential therapeutic target for obesity and type 2 diabetes.
化学数据
分子量 | 437.49 |
分子式 | C27H23N3O3 |
CAS号 | 947669-91-2 |
纯度 | >98% |
溶解性(25°C) | DMSO: 5 mg/mL clear (warmed) |
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 | 2.2858 mL | 11.4288 mL | 22.8577 mL |
5 mM | 0.4572 mL | 2.2858 mL | 4.5715 mL |
10 mM | 0.2286 mL | 1.1429 mL | 2.2858 mL |