生物活性
Neurotensin is a gut tridecapeptide with many central and peripheral functions, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors(NTR). Neurotensin induces the expression of MIP-2, MCP-1, IL-1β and TNFα in murine microglial cells and stimulates IL-8 secretion in a non-transformed colon epithelial cell line stably transfected with the NTR. The high-affinity NTR, a member of the G-protein coupled receptor (GPCR) family, is present in a majority of human pancreatic and colorectal cancers, suggesting that Neurotensin (NT) may act in an endocrine fashion to affect tumor growth. Acting through the NTR1, Neurotensin is known to stimulate various signal transduction pathways, including intracellular calcium ([Ca2+]i), the mitogen-activated protein kinases (MAPKs), ERK and JNK, and various PKC isoforms. Treatment of HCT116 cells with Neurotensin (100 nM) significantly increases HCT116 cell migration (~3-fold) compared with vehicle treatment.
化学数据
分子量 | 1672.92 |
分子式 | C78H121N21O20 |
CAS号 | 39379-15-2 |
纯度 | >97% |
溶解性(25°C) | Water 30 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 | 0.5978 mL | 2.9888 mL | 5.9776 mL |
5 mM | 0.1196 mL | 0.5978 mL | 1.1955 mL |
10 mM | 0.0598 mL | 0.2989 mL | 0.5978 mL |