P8RI (D-P8RI) peptide

P8RI (D-P8RI) peptide

• COA/MS/HPLC Report
• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

kwpalfvr

H-kwpalfvr-OH

8

99.02%

C₅₁H₇₇N₁₃O₉

1016.24

2147724-76-1

162678845

Synthetic

Powder

P8RI(CD31 agonist), a retro-inverso sequence of the best candidate identified by functional in vitro screening of a peptide library, passed an absorption, distribution, metabolism, excretion and toxicology analysis. The IC50 of P8RI based on the human ether-a-go-go-related gene tail current amplitude was 150 μg/ml, which represents an ≈40-fold Cmax of the drug in the plasma of subcutaneously injected mice. Of note, at the concentration of 5 μg/ml, which is higher than the Cmax in the blood after subcutaneous injection, the peptide has no effect on the tail amplitude of the potassium channel. P8RI significantly affected the polarization of macrophages, resulting in a dramatic reduction in M1 markers such as the expression of iNOS and arginase II and the production of IL-6, IL-12p70, and TNF-α, whereas it enhanced the M2 phenotype, as detected by an increased expression of arginase I and production of IL-10. Curative treatment with P8RI promotes the healing of experimental dissecting aneurysm in atherosclerotic mice.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual: Handling and Storage of Synthetic Peptides

• Vigne, J., Bay, S., Aid-Launais, R. et al. Cleaved CD31 as a target for in vivo molecular imaging of inflammation. Sci Rep 9, 19560 (2019). https://doi.org/10.1038/s41598-019-56163-x

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.