PeptideDB

TP508 TFA

TP508 TFA

CAS No.:

TP508 TFA is a 23 amino acid (AA) non-proteolytic thrombin peptide that represents part of the receptor-binding domain o
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This product is for research use only, not for human use. We do not sell to patients.

TP508 TFA is a 23 amino acid (AA) non-proteolytic thrombin peptide that represents part of the receptor-binding domain of the thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates NO production in human endothelial cells. TP508 TFA regenerates blood vessels and tissues by activating endothelial cells and stem cells.

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
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.