Physicochemical Properties
| Molecular Formula | C??H???N??F?O??S |
| Molecular Weight | 2426.46 |
| Related CAS # | TP508;121341-81-9 |
| Appearance | White to off-white solid powder |
| Synonyms | TP508 TFA; TP508 TFA |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | TP508 (50 μg/mL; 24 h; HCAEC) therapy restored radiation-induced endothelial dysfunction (ED) and loss of NO signaling by attenuating eNOS downregulation. TP508 therapy can enhance NO generation in irradiated cells[1]. TP508 reduces the effects of nuclear radiation on cultured human endothelial cells, increases endothelial NO generation, promotes tube formation, and speeds up the repair of radiation-induced DNA double-strand breaks (DSB) [1]. TP508 is a thrombin antagonist that suppresses its actions via RGD and αvβ3-related pathways [3]. |
| ln Vivo | When injected 24 hours after 8.5 Gy of irradiation, TP508 (10 mg/kg; i.v.; male CD-1 mice) therapy dramatically increased the lifespan of CD-1 animals and prevented radiation-induced endothelial cell damage [1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: Primary human coronary artery endothelial cells (HCAEC) Tested Concentrations: 50 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Prevented the radiation-induced downregulation of eNOS. |
| Animal Protocol |
Animal/Disease Models: Male CD-1 mice (12-15-week old) with γ irradiation[1] Doses: 10 mg/kg Route of Administration: intravenous (iv) injection Experimental Results: Mitigated radiation-induced endothelial cell damage, also Dramatically increased survival of CD-1 mice. |
| References |
[1]. 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]. 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]. 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. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (41.21 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |