TP508 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 可激活内皮NO synthase (eNOS)并刺激人内皮细胞中 NO 的产生。TP508 通过激活内皮细胞和干细胞以使血管再生和组织再生。
| 生物活性 | TP508 is a 23-amino acid nonproteolyticthrombinpeptide that represents a portion of the receptor-binding domain ofthrombinmolecule. TP508 activates endothelialNO synthase(eNOS)and stimulates production of NO in human endothelial cells. TP508 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].
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. |
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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].
| 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. |
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| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 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 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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