Neurotensin(8-13)是神经降压素（Neurotensin）的核心活性片段，Neurotensin(8-13)是具有生物活性的神经降压素受体（NTSR1）激动剂，通过与NTSR1高亲和力结合（Kd≈1-10nM）激活Gq/11蛋白信号通路，进而调控细胞内钙离子浓度及蛋白激酶C（PKC）的活性。
Cas No.:60482-95-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Neurotensin(8-13) is the core active fragment of neurotensin and functions as a biologically active neurotensin receptor (NTSR1) agonist. By binding to NTSR1 with high affinity (Kd≈1–10nM), Neurotensin(8-13) activates the Gq/11 protein signaling pathway, thereby regulating intracellular calcium ion concentration and the activity of protein kinase C (PKC)[1-2]. Neurotensin(8-13) can be used in research related to pain management, psychiatric disorders (such as schizophrenia and depression), and tumor-targeted therapy[3-4].
In vitro, human colon adenocarcinoma HT-29 cells were treated with Neurotensin(8-13) (3–100nM) for 1–2 hours. Neurotensin(8-13) significantly induced rapid internalization mediated by the neurotensin receptor NTR1 and caused a time-dependent downregulation of NTR1 receptors on the cell surface[5]. Human non-small cell lung cancer cells NCI-H1299 were treated with Neurotensin(8-13) (100nM) for 2.5 minutes, which significantly induced tyrosine phosphorylation of focal adhesion kinase (FAK). After treating NCI-H1299 cells with Neurotensin(8-13) (10nM) for 24 hours, Neurotensin(8-13) promoted the proliferation of NCI-H1299 cells[6].
In vivo, normotensive rats were injected via the femoral vein with Neurotensin(8-13) (0.1–100nmol/kg). Neurotensin(8-13) dose-dependently reduced diastolic and systolic blood pressure without altering heart rate and showed no direct vasodilatory effect on isolated rat aortic rings[7]. Male Long-Evans rats received microinjections of Neurotensin(8-13) (3nmol in 0.5μl) into the ventral midbrain tegmental area. Neurotensin(8-13) significantly enhanced the reward effect of brain stimulation in the midbrain central gray matter 15–55 minutes after injection[8].
References:
[1] Gilbert JA, McCormick DJ, Pfenning MA, et al. Neurotensin(8-13): comparison of novel analogs for stimulation of cyclic GMP formation in neuroblastoma clone N1E-115 and receptor binding to human brain and intact N1E-115 cells. Biochem Pharmacol. 1989 Oct 1;38(19):3377-82.
[2] Cocioabă D, Fonseca AI, Leonte R, et al. Neurotensin (8-13) and Neuromedin N Neuropeptides Radiolabelling with Copper-64 Produced on Solid or Liquid Targets. Molecules. 2024 Mar 20;29(6):1390.
[3] Li XM, Von Euler G, Hedlund PB, et al. The C-terminal neurotensin-(8-13) fragment potently modulates rat neostriatal dopamine D2 receptors. Eur J Pharmacol. 1993 Mar 30;234(1):125-8.
[4] Pinnock RD, Woodruff GN. The non-peptide neurotensin receptor antagonist SR48692 is not a potent antagonist of neurotensin(8-13) responses of rat substantia nigra neurones in vitro. Neurosci Lett. 1994 May 19;172(1-2):175-8.
[5] García-Garayoa E, Bläuenstein P, Bruehlmeier M, 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.
[6] Leyton J, Garcia-Marin L, Jensen RT, et al. Neurotensin causes tyrosine phosphorylation of focal adhesion kinase in lung cancer cells. Eur J Pharmacol. 2002 May 10;442(3):179-86.
[7] Di Paola ED, Richelson E. Cardiovascular effects of neurotensin and some analogues on rats. Eur J Pharmacol. 1990 Jan 17;175(3):279-83.
[8] Rompré PP, Gratton A. Mesencephalic microinjections of neurotensin-(1-13) and its C-terminal fragment, neurotensin-(8-13), potentiate brain stimulation reward. Brain Res. 1993 Jul 9;616(1-2):154-62.
Neurotensin(8-13)是神经降压素（Neurotensin）的核心活性片段，Neurotensin(8-13)是具有生物活性的神经降压素受体（NTSR1）激动剂，通过与NTSR1高亲和力结合（Kd≈1-10nM）激活Gq/11蛋白信号通路，进而调控细胞内钙离子浓度及蛋白激酶C（PKC）的活性[1-2]。Neurotensin(8-13)可用于疼痛管理、精神疾病（如精神分裂症、抑郁症）及肿瘤靶向治疗的相关研究[3-4]。
在体外，Neurotensin(8-13)（3-100nM）处理人结肠腺癌HT-29细胞1-2小时，Neurotensin(8-13)显著诱导神经降压素受体NTR1介导的快速内化，并引起细胞表面NTR1受体的时间依赖性下调[5]。Neurotensin(8-13)（100nM）处理人非小细胞肺癌细胞NCI-H1299 2.5分钟，可显著诱导黏着斑激酶（FAK）的酪氨酸磷酸化。Neurotensin(8-13)（10nM）处理NCI-H1299细胞24小时能促进NCI-H1299细胞增殖[6]。
在体内，Neurotensin(8-13)经股静脉注射处理正常血压大鼠（0.1-100nmol/kg），Neurotensin(8-13)以剂量依赖方式降低舒张压和收缩压，但不改变心率，且对离体大鼠主动脉环无直接血管舒张作用 [7]。Neurotensin(8-13)经中脑腹内侧被盖区微注射（3nmol; 5μl）处理雄性Long-Evans大鼠，Neurotensin(8-13)在注射后15-55分钟显著增强中脑中央灰质脑刺激奖励效应[8]。
| Cell experiment [1]: | |
Cell lines | NCI-H1299 cells (human non-small cell lung cancer cell line) |
Preparation Method | NCI-H1299 cells were maintained in RPMI-1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with Neurotensin(8-13) at concentrations ranging from 1nM to 1μM for 2.5 minutes to 24 hours. |
Reaction Conditions | 1nM to 1μM; 2.5 minutes to 24 hours |
Applications | Neurotensin(8-13) induced transient tyrosine phosphorylation of focal adhesion kinase (FAK) in NCI-H1299 cells, with maximal phosphorylation observed 1–2.5 minutes after treatment. This effect was specific to the C-terminal fragment. The tyrosine phosphorylation was inhibited by the nonpeptide neurotensin receptor antagonist SR48692 (10μM). Neurotensin(8-13) also bound with high affinity to NCI-H1299 cells (IC₅₀=10nM) and stimulated clonal growth in soft agar assays, while SR48692 suppressed proliferation. |
| Animal experiment [2]: | |
Animal models | Normotensive rats |
Preparation Method | Rats were anesthetized with Pentobarbital (55mg/kg; i.p.), and a cannula was inserted into the femoral vein for peptide administration. Neurotensin(8-13) was dissolved in 0.9% NaCl and injected intravenously at doses ranging from 0.1 to 100nmol/kg. Blood pressure and heart rate were monitored via the carotid artery. |
Dosage form | 0.1–100nmol/kg; i.v.; Single injection. |
Applications | Neurotensin(8-13) induced a dose-dependent decrease in diastolic blood pressure (ED₅₀=6.0nmol/kg) without altering heart rate. At higher doses (≥3nmol/kg), Neurotensin(8-13) elicited a triphasic depressor-pressor-depressor response, with effects lasting over 40 minutes at the highest dose (100nmol/kg). Tachyphylaxis was observed upon repeated administration. |
References: | |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.224 mL | 6.12 mL | 12.2401 mL |
| 5 mM | 244.8 μL | 1.224 mL | 2.448 mL |
| 10 mM | 122.4 μL | 612 μL | 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet