TP508 TFA

TP508 TFA; 纯度: 99.79%

TP508 TFA 是一种 23 个氨基酸的非蛋白水解凝血酶肽,代表凝血酶分子受体结合结构域的一部分。TP508 TFA 可激活内皮 NO synthase (eNOS) 并刺激人内皮细胞中 NO 的产生。TP508 TFA 通过激活内皮细胞和干细胞以使血管再生和组织再生。

TP508 TFA 

TP508 TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
50 mg ¥16500 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

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TP508 TFA 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues[1][2].

体外研究
(In Vitro)

TP508 (50 μg/mL; 24 hours; HCAEC) treatment reverses radiation-induced endothelial dysfunction (ED) and loss of NO signaling by attenuating the downregulation of eNOS expression. TP508 treatment is able to stimulate NO production in the irradiated cells[1].
TP508 mitigates effects of nuclear radiation on human endothelial cells in culture restoring endothelial NO production, tube formation and accelerating repair of radiation-induced DNA double-strand breaks (DSB)[1].
TP508 acts as an antagonist for the effects of thrombin. TP508 peptide inhibits these thrombin-induced effects through a RGD and αvβ3-related mechanism[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Primary human coronary artery endothelial cells (HCAEC)
Concentration: 50 μg/mL
Incubation Time: 24 hours
Result: Prevented the radiation-induced downregulation of eNOS.

体内研究
(In Vivo)

TP508 (10 mg/kg; intravenous injection; male CD-1 mice) treatment mitigates radiation-induced endothelial cell damage, also significantly increases survival of CD-1 mice when injected 24 h after 8.5 Gy exposure[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice (12-15-week old) with γ irradiation[1]
Dosage: 10 mg/kg
Administration: Intravenous injection
Result: Mitigated radiation-induced endothelial cell damage, also significantly increased survival of CD-1 mice.

Clinical Trial

分子量

2426.46

Formula

C99H147N28F3O38S

Sequence

Ala-Gly-Tyr-Lys-Pro-Asp-Glu-Gly-Lys-Arg-Gly-Asp-Ala-Cys-Glu-Gly-Asp-Ser-Gly-Gly-Pro-Phe-Val

Sequence Shortening

AGYKPDEGKRGDACEGDSGGPFV

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 50 mg/mL (20.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.4121 mL 2.0606 mL 4.1212 mL
5 mM 0.0824 mL 0.4121 mL 0.8242 mL
10 mM 0.0412 mL 0.2061 mL 0.4121 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

参考文献
  • [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]. 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.