Cortistatin-14 (trifluoroacetate salt)
目录号 : GC43311
A neuropeptide agonist of somatostatin receptors
Sample solution is provided at 25 µL, 10mM.
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Cortistatin-14 is an endogenous neuropeptide agonist of somatostatin receptors (IC50s = 0.5-18.2 nM for human SST1-SST5 receptors expressed in CCL39 cells).[1],[2] It is expressed in GABAergic interneurons in the cortex and hippocampus.[2],[3] Cortistatin-14 competitively inhibits hexarelin binding to human growth hormone secretagogue receptors (GHS-R) in pituitary membranes (Ki = 0.54 μM).[4] It also activates the human Mas-related gene receptor MrgX2 expressed in HEK293 cells leading to quantifiable GTP-γS binding to the G protein subunit Gαο (EC50 = 1.3 μM).[5] Cortistatin-14 (0.01-1 μM), similarly to somatostatin-14, completely inhibits thyrotropin-releasing hormone, and partially inhibits vasoactive intestinal peptide, stimulation of cAMP production in GH4 cells.[3] In mice, cortistatin-14 dose-dependently (0.05-5 μg, i.c.v.) impairs memory retention when administered after foot shock avoidance training.[6] Cortistatin-14 (40-320 μg/kg, s.c.) dose-dependently reduces growth hormone secretion in rats by greater than 80% after 10 minutes when administered at doses of 40-320 µg/kg.[7]
Reference:
[1]. Criado, J.R., Li, H., Jiang, X., et al. Structural and compositional determinants of cortistatin activity. J. Neurosci. Res. 56(6), 611-619 (1999).
[2]. Spier, A.D., and de Lecea, L. Cortistatin: A member of the somatostatin neuropeptide family with distinct physiological functions. Brain Res. Brain Res. Rev. 33(2-3), 228-241 (2000).
[3]. de Lecea, L., Criado, J.R., Prospero-Garcia, O., et al. A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature 381(6579), 242-245 (1996).
[4]. Deghenghi, R., Papotti, M., Ghigo, E., et al. Cortistatin, but not somatostatin, binds to growth hormone secretagogue (GHS) receptors of human pituitary gland. J. Endocrinol. Invest. 24(1), RC1-RC3 (2001).
[5]. Burstein, E.S., Ott, T.R., Feddock, M., et al. Characterization of the Mas-related gene family: structural and functional conservation of human and rhesus MrgX receptors. Br. J. Pharmacol. 147(1), 73-82 (2006).
[6]. Flood, J.F., Uezu, K., and Morley, J.E. The cortical neuropeptide, cortistatin-14, impairs post-training memory processing. Brain Res. 775(1-2), 250-252 (1997).
[7]. Deghenghi, R., Avallone, R., Torsello, A., et al. Growth hormone-inhibiting activity of cortistatin in the rat. J. Endocrinol. Invest. 24(11), RC31-RC33 (2001).
| Cas No. | SDF | ||
| 化学名 | L-prolyl-L-cysteinyl-L-lysyl-L-asparaginyl-L-phenylalanyl-L-phenylalanyl-L-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-L-seryl-L-seryl-L-cysteinyl-L-lysine, cyclic (2→13)-disulfide, trifluoroacetate salt | ||
| Canonical SMILES | [H]N1CCC[C@H]1C(N[C@H](C(N[C@@H](CCCCN)C(N[C@@H](CC(N)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CCCCN)C(N[C@]([C@@H](C)O)([H])C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CO)C2=O)=O)=O)CC3=CC=CC=C3)=O)=O)=O)CC4=CNC5=C4C=CC=C5)=O)CC6=CC=CC=C6)=O)CC7=CC=CC=C7)=O)=O)=O)CSS | ||
| 分子式 | C81H113N19O19S2 • XCF3COOH | 分子量 | 1721 |
| 溶解度 | 1mg/mL in water | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.5811 mL | 2.9053 mL | 5.8106 mL |
| 5 mM | 0.1162 mL | 0.5811 mL | 1.1621 mL |
| 10 mM | 0.0581 mL | 0.2905 mL | 0.5811 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
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet