生物活性
COG 133 is a fragment of Apolipoprotein E (APOE) peptide with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM. COG 133 (0.02, 0.2, and 2.0 μM) improved cell numbers in glutamine free media. In IEC-6 cells, COG 133 (0.2-20 μM) improved cell migration following 5-FU challenge, reaching the same migration level as controls. COG 133 (3 μM) significantly increased the mitotic crypt numbers in C57BL6J wild-type animals. COG 133 treatment improved crypt architecture and reduced lamina propria inflammation. COG 133 (3 μM) significantly reduced the intestinal MPO levels. COG 133 partially decreased TNF-α level in the proximal small intestine from 5-FU-treated mice. In both wild-type and ApoE knock-out mice, COG 133 (3 μM) reverted the increase in Tunel-positive cells in the proximal intestine induced by 5-FU. COG 133 caused higher expression of the NF-κB in the improved intestinal mucosa.
化学数据
分子量 | 2169.71 |
分子式 | C97H181N37O19 |
CAS号 | 514200-66-9 |
纯度 | >98% |
溶解性(25°C) | Water 1 mg/mL |
储存和运输条件 | -20°C, sealed 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 | 0.4609 mL | 2.3045 mL | 4.6089 mL |
5 mM | 0.0922 mL | 0.4609 mL | 0.9218 mL |
10 mM | 0.0461 mL | 0.2304 mL | 0.4609 mL |