THR-184 peptide (TFA removed)

THR-184 peptide (TFA removed)

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

Batch to batch variation of the purity

H-CYYDNSSSVLCKRYRS-OH, (Cys1-Cys11 disulfide bond)

H-Cys-Tyr-Tyr-Asp-Asn-Ser-Ser-Ser-Val-Leu-Cys-Lys-Arg-Tyr-Arg-Ser-OH (C1-C11 disulfide bond)

16

95.06%

C₈₂H₁₂₄N₂₄O₂₇S₂

1942.13

Synthetic

Powder

THR-184 is an agonist of BMP signaling and a potent antagonist of TGFβ signaling. This small peptide mimetic inhibits inflammation, apoptosis, and fibrosis and reverses epithelial-to-mesenchymal transition (EMT) by regulating multiple signaling pathways involved in the cellular injury of multiple organs. Its effects have been shown to control Acute Kidney Injury (AKI). THR-184 has progressed through phase I and II clinical trials to prevent cardiovascular surgery (CVS) associated with AKI. This work provides a roadmap for developing other growth factor mimetics and demonstrates how we might harness their therapeutic potential.

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

• Carlson WD, Keck PC, Bosukonda D, Carlson FR Jr. A Process for the Design and Development of Novel Bone Morphogenetic Protein-7 (BMP-7) Mimetics With an Example: THR-184. Front Pharmacol. 2022 Jul 8;13:864509.

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.