生物活性
G3335 ( L-tryptophyl-L-glutamic acid) is a cell-permeable dipeptide that acts as a selective and reversible PPARγ antagonist with a Kd value of 8.34 μM for PPARγ and much lower activity at other PPAR subtypes. G3335 reversibly and competitively blocks activation of PPARγ by the PPARγ agonist rosiglitazone, and conversely, in rat astrocyte culture higher levels of rosiglitazone reduced harmful effects induced by G3335. At higher concentration G3335 may act as a PPARα agonist, interacting with the PPARα ligand binding domain with a KD of 120 μM. G3335 is reported to reduce hepatic lipid accumulation in lipid-loaded hepatocytes by activation of PPARα.
化学数据
分子量 | 333.34 |
分子式 | C16H19N3O5 |
CAS号 | 36099-95-3 |
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 | 2.9999 mL | 14.9997 mL | 29.9994 mL |
5 mM | 0.6 mL | 2.9999 mL | 5.9999 mL |
10 mM | 0.3 mL | 1.5 mL | 2.9999 mL |