Pegtarazimod  (Synonyms: RLS-0071)

Pegtarazimod (RLS-0071) is a dual-target anti-inflammatory peptide that exerts its effects by simultaneously regulating the complement system and neutrophil-associated inflammatory pathways. Pegtarazimod reduces ROS production both in vitro and in vivo, and decreases the level of neutrophil elastase, a marker of neutrophil extracellular traps (NETs), in vivo, thereby alleviating inflammatory responses. Pegtarazimod significantly improves the survival rate of mice in multiple in vivo models of acute graft-versus-host disease (aGVHD). Pegtarazimod inhibits the activation of the C1 complex, reduces the herpes zoster-like spread of herpes simplex virus type 1 skin infection, and improves the survival rate of infected mice. Pegtarazimod can be used in research related to acute graft-versus-host disease, acute pulmonary diseases, and skin herpes simplex virus type 1 infection^[1][2][3].

Pegtarazimod reduces reactive oxygen species (ROS) production in an unspecified in vitro cell system^[1].
Pegtarazimod (0.3-2.8 mg/mL) inhibits classical complement pathway activation in spiked normal human plasma in a dose-dependent manner, with 40% inhibition at 0.3 mg/mL and over 80% inhibition at 2.8 mg/mL^[2].
Pegtarazimod (0.3-22 mg/mL; 30 min (neutrophil incubation at room temperature); 2 h (CCK-8 dye incubation at 37 °C)) increases the survival of purified human neutrophils ex vivo in a dose-dependent manner^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pegtarazimod (14.4 mM (40 mg/mL); topical; twice daily; 14 days) formulated in HEC gel provides 53.3% survival in GFP-HSV-1-infected BALB/cJ mice over 14 days, significantly reduces infection severity, and promotes lesion healing^[3].
Pegtarazimod (14.4 mM (40 mg/mL); topical; twice daily; 14 days) formulated in HEC gel significantly reduces vesicle formation and promotes complete lesion healing by day 12 in ACVR-HSV-1-infected BALB/cJ mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

2771.32

C₁₂₂H₂₂₄N₂₀O₄₆S₂

2056232-82-5

Ile-Ala-Leu-Ile-Leu-Glu-Pro-Ile-Cys-Cys-Gln-Glu-Arg-Ala-Ala-{PEG24}

IALILEPICCQERAA-{PEG24}

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Verena Holzmüller, et al. Exploring a Novel Anti-Inflammatory Peptide As a Potential Treatment for Acute Graft-Versus-Host Disease (aGVHD). Volume 144, Supplement 1, 5 November 2024, Page 3399

  [2]. Jessica Goss, et al. RLS-0071, a dual-targeting anti-inflammatory peptide - biomarker findings from a first in human clinical trial. Volume 8, article number 1, (2023)

  [3]. Bhutta MS, et al. Peptide Inhibitor of Complement C1, RLS-0071, Reduces Zosteriform Spread of Herpes Simplex Virus Type 1 Skin Infection and Promotes Survival in Infected Mice. Viruses. 2021;13(8):1422. Published 2021 Jul 22.  [Content Brief]