TP508
目录号 : GC34255
TP508是由23个氨基酸残基构成的多肽，它代表了人凝血素的第508-530位氨基酸序列，被认为是高亲和性受体与凝血素的结合域。
Cas No.:121341-81-9
Sample solution is provided at 25 µL, 10mM.
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TP508 is a 23 amino acid synthetic peptide representing residues 508-530 of human prothrombin which is identified as a potential receptor-binding domain based on competition for high-affinity thrombin binding to fibroblasts.
TP508 treatment reverses radiation effects on NO signaling, restores tube formation and accelerates the repair of radiation-induced DSB in irradiated human endothelial cells[1]. TP508 injection increases responsiveness of endothelial cells from aortic explants to VEGF-stimulated angiogenesis in vitro. TP508 stimulation does not significantly affect the VEGF mRNA levels in normoxic or hypoxic cells[2]. TP508 acts as an antagonist for the effects of thrombin. TP508 peptide inhibits these thrombin-induced effects through a RGD and αvβ3-related mechanism[4].
TP508 (500 μg) in sham-irradiated animals significantly increases the amount of endothelial cell sprouting from aortic explants. TP508 significantly increases the sprouting in sham-irradiated and irradiated animals, more than doubling the amount of sprouting in explants from animals at all exposure doses. TP508 (10 mg/kg) given 24 h after 8.5 Gy gamma irradiation significantly increases 30-day survival in mice, from 26.7 to 73.3%[1]. TP508 injection increases endothelial sprouting and potentiates VEGF-stimulated angiogenesis[2]. In type I diabetic swine, TP508 (1 mg/kg, infusion) reduces infarct size after IR[3].
[1]. Olszewska-Pazdrak B, et al. Nuclear Countermeasure Activity of TP508 Linked to Restoration of Endothelial Function and Acceleration of DNA Repair. Radiat Res. 2016 Aug;186(2):162-74. [2]. Olszewska-Pazdrak B, et al. Systemic administration of thrombin peptide TP508 enhances VEGF-stimulated angiogenesis and attenuates effects of chronic hypoxia. J Vasc Res. 2013;50(3):186-9 [3]. Chu LM, et al. Effect of thrombin fragment (TP508) on myocardial ischemia reperfusion injury in a model of type 1 diabetes mellitus. Circulation. 2010 Sep 14;122(11 Suppl):S162-9. [4]. Tsopanoglou NE, et al. On the mode of action of thrombin-induced angiogenesis: thrombin peptide, TP508, mediates effects in endothelial cells via alphavbeta3 integrin. Thromb Haemost. 2004 Oct;92(4):846-57.
Animal experiment: | Mice: One hour after irradiation, mice are placed in a restrainer and intravenously (i.v.) injected through the tail vein with a single dose of TP508 in 100 μL sterile saline or 100 μL sterile saline alone. After 24 h, the mice are euthanized by CO2 inhalation and thoracic aortas are isolated from TP508- or saline-alone treated mice and transferred to culture dishes containing cold sterile EBM. The periaortic fibro-adipose tissue is removed under a dissecting microscope and aortas are rinsed with cold EBM and cut transversely to create 1 mm aortic rings (appr 10 per aorta). Aortic rings are cut, opened, and the inner endothelial surface is placed directly on Matrigel matrix-coated 24-well plates. Aortic explants are cultured in a 5% CO2 atmosphere at 37°C in EGM containing 5% FBS and SingleQuots endothelial growth factors. Endothelial cell sprouting is monitored daily by inverted phase contrast microscopy and images are captured using SPOT RT camera and advanced imaging software at 40× and 100× magnification. |
References: [1]. Olszewska-Pazdrak B, et al. Nuclear Countermeasure Activity of TP508 Linked to Restoration of Endothelial Function and Acceleration of DNA Repair. Radiat Res. 2016 Aug;186(2):162-74. | |
| Cas No. | 121341-81-9 | SDF | |
| Canonical SMILES | Ala-Gly-Tyr-Lys-Pro-Asp-Glu-Gly-Lys-Arg-Gly-Asp-Ala-Cys-Glu-Gly-Asp-Ser-Gly-Gly-Pro-Phe-Val | ||
| 分子式 | C97H146N28O36S | 分子量 | 2312.44 |
| 溶解度 | Soluble 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.4324 mL | 2.1622 mL | 4.3244 mL |
| 5 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL |
| 10 mM | 0.0432 mL | 0.2162 mL | 0.4324 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