Neurotensin(8-13)
(Synonyms: 神经降压素(8-13)) 目录号 : GC36729
A neuropeptide
Cas No.:60482-95-3
Sample solution is provided at 25 µL, 10mM.
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Neurotensin (8-13) is a neuropeptide that corresponds to the C-terminal residues 8-13 of neurotensin that binds to rat synaptic membranes with a Ki value of 13 nM.1 It induces contraction of guinea pig ileum (EC50 = 25 nM) and induces contraction of rat fundus equipotently to full length neurotensin (EC50s = 1.29 and 1.58 nM, respectively).1,2 In vivo, neurotensin (8-13) has antinociceptive effects in a mouse tail pressure test (ED50 = 50 nmol per animal).3 It induces extracellular dopamine release in the prefrontal cortex in rats.4 Neurotensin (8-13) also decreases diastolic blood pressure in a dose-dependent manner in normotensive rats without affecting heart rate.5
1.Granier, C., van Rietschoten, J., Kitabgi, P., et al.Synthesis and characterization of neurotensin analogues for structure/activity relationship studies. Acetyl-neurotensin-(8--13) is the shortest analogue with full binding and pharmacological activitiesEur. J. Biochem.124(1)117-124(1982) 2.Huidobro-Toro, J.P., and Kullak, A.Excitatory neurotensin receptors on the smooth muscle of the rat fundus: Possible implications in gastric motilityBr. J. Pharmacol.84(4)897-910(1985) 3.Furuta, S., Kisara, K., Sakurada, S., et al.Structure-antinociceptive activity studies with neurotensinBr. J. Pharmacol.83(1)43-48(1984) 4.Sotty, F., Brun, P., Leonetti, M., et al.Comparative effects of neurotensin, neurotensin(8-13) and [D-Tyr11]neurotensin applied into the ventral tegmental area on extracellular dopamine in the rat prefrontal cortex and nucleus accumbensNeuroscience98(3)485-492(2000) 5.Di Paola, E.D., and Richelson, E.Cardiovascular effects of neurotensin and some analogues on ratsEur. J. Pharmacol.175(3)279-283(1990)
Kinase experiment: | Binding assays are performed on whole HT-29 cells at confluence. A day before the assay, cells (106 cells/0.4 mL, equivalent to 0.3 mg protein) are placed in 48-well plates. A special binding buffer that includes protease inhibitors (50 mM HEPES, 125 mM NaCl, 7.5 mM KCl, 5.5 mM MgCl2, 1 mM EGTA, 5 g/L bovine serum albumin, 2 mg/L chymostatin, 100 mg/L soybean trypsin inhibitor, 50 mg/L bacitracin, pH 7.4) is used for the experiments. In inhibition studies, cells are incubated for 1 h at 37°C in triplicate with 25,000 cpm of 125I-NT and variable concentrations (0.001-3,000 nM) of unlabeled NT(8-13), unlabeled NT-VIII, or NT-VIII labeled with natRe (final volume of 0.2 mL per well). The cells are then washed twice with cold binding buffer and afterward are solubilized with 1N NaOH at 37°C (0.4 mL per well). The activity is determined in a γ-counter. In saturation studies, cells are incubated in triplicate with increasing concentrations (0.1-10 nM) of 99mTc(CO)3NT-VIII for 1 h at 37°C (final volume, 0.2 mL per well). The concentrations of total technetium (99+99mTc) are equivalent to 0.2-20 MBq 99mTc activity per well. After 2 washings with the same binding buffer as before, the cells are then solubilized with 1N NaOH at 37°C (0.4 mL per well). The bound radioactivity is measured in the γ-counter. Nonspecific binding is determined with 1 μM unlabeled NT(8-13)[1]. |
References: [1]. García-Garayoa E, et al. Preclinical evaluation of a new, stabilized neurotensin(8--13) pseudopeptide radiolabeled with (99m)tc. J Nucl Med. 2002 Mar;43(3):374-83. | |
| Cas No. | 60482-95-3 | SDF | |
| 别名 | 神经降压素(8-13) | ||
| 分子式 | C38H64N12O8 | 分子量 | 816.99 |
| 溶解度 | Water: 50 mg/mL (61.20 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.224 mL | 6.12 mL | 12.2401 mL |
| 5 mM | 0.2448 mL | 1.224 mL | 2.448 mL |
| 10 mM | 0.1224 mL | 0.612 mL | 1.224 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet