TB-500 10mg

Compound Name: TB-500 (Ac-Tβ4(17–23))

Synonyms: TB500, 885340-08-9, UNII-QHK6Z47GTG, QHK6Z47GTG, TB-500

CAS Number: 77591-33-4

Molecular Formula: C₂₁₂H₃₅₀N₅₆O₇₈S

Molecular Weight: ~4963 g/mol

Structure: Synthetic acetylated 7-amino acid peptide derived from Tβ4

Peptide Sequence: Ac-Leu-Lys-Lys-Thr-Glu-Thr-Gln-OH

Chemical Structure:

Source: PubChem

Mechanism of Action: TB-500 mimics the bioactive region of thymosin β4, interacting with actin monomers to regulate the cytoskeleton¹. It promotes cell migration, angiogenesis, and wound re-epithelialization. Research suggests TB-500’s effects may also be mediated through its metabolite Ac-LKKTE^2,3.

Biological Activity: Demonstrates potent pro-regenerative, pro-angiogenic, and anti-inflammatory properties. TB-500 enhances keratinocyte and fibroblast migration, accelerates dermal healing, and supports vascularization in injured tissues without cytotoxicity^1-4.

Storage: Store lyophilized powder at –20°C. Reconstituted solutions should be stored at 2–8°C and used within 30 days.

Drug Categories: Peptide therapeutic, wound healing agent, angiogenesis modulator

Additional Notes:

• Under investigation for use in cardiac, corneal, and dermal tissue repair.
• Subject to anti-doping regulations due to performance-enhancing properties.

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

TB-500 is a synthetic peptide designed to replicate the wound healing and regenerative functions of thymosin β4. Composed of seven amino acids, TB-500 corresponds to the bioactive region (LKKTETQ) of thymosin β4, with an N-terminal acetylation to improve stability and bioavailability. Studies suggest that TB-500 plays a key role in modulating actin polymerization, thereby supporting cytoskeletal reorganization during tissue repair. It has shown effectiveness in models of corneal, dermal, and cardiac injuries^1,3,4. In vitro and in vivo research has demonstrated that TB-500 and its metabolites are non-cytotoxic, with the Ac-LKKTE metabolite particularly enhancing fibroblast-driven wound closure. TB-500 continues to be of interest in regenerative medicine research, despite its inclusion on the World Anti-Doping Agency’s prohibited list.

Research Highlights

• Promotes dermal and tendon healing via fibroblast recruitment³
• Promotes blood vessel formation, aiding ischemic tissue recovery⁴
• Modulates cytoskeletal remodeling critical for cell migration and repair¹
• Demonstrated safety in cellular assays across multiple tissues.²
• Ac-LKKTE, a TB-500 metabolite, exhibits superior activity in promoting wound closure compared to the parent compound³.

Mechanism of Action

TB-500 exerts its effects by mimicking the actin-sequestering function of thymosin β4. Through its interaction with G-actin monomers, TB-500 regulates actin polymerization essential for cell motility and wound closure. The peptide enhances fibroblast and keratinocyte migration, promotes new capillary formation, and supports tissue matrix remodeling^1-3. Notably, its metabolite Ac-LKKTE has been identified as a key driver of wound-healing efficacy in vitro, highlighting the importance of peptide metabolism in therapeutic applications^3,4.

Pharmacokinetic Profile:

• Route of Administration: subcutaneous (experimental)
• Half-Life: Short (~30-90 min); dependent on route and formulation
• Formulation: Lyophilized powder for reconstitution

Formulation & Handling

• Lyophilized peptide powder, reconstituted in sterile PBS or water.
• Store lyophilized form at –20 °C; Store reconstituted solution at 2-8°C and use within 30 days.
• Avoid repeated freeze–thaw cycles.

Selected Clinical Trial Activity

References

¹Treadwell, T., Kleinman, H. K., Crockford, D., Hardy, M. A., Guarnera, G. T. & Goldstein, A. L. The regenerative peptide thymosin β4 accelerates the rate of dermal healing in preclinical animal models and in patients. Ann. N. Y. Acad. Sci. 1270, 37–44 (2012).

²Rahaman, K. A. et al. Simultaneous quantification of TB-500 and its metabolites in in-vitro experiments and rats by UHPLC-Q-Exactive orbitrap MS/MS and their screening by wound healing activities in-vitro. J. Chromatogr. B 1235, 124033 (2024).

³Maar, K. et al. Utilizing developmentally essential secreted peptides such as thymosin beta-4 to remind the adult organs of their embryonic state—new directions in anti-aging regenerative therapies. Cells 10, 1343 (2021).

⁴Sosne, G. et al. Thymosin beta 4 promotes corneal wound healing and decreases inflammation in vivo following alkali injury. Exp. Eye Res. 74, 293–299 (2002).