Protegrin-1  (Synonyms: PG1)

Protegrin-1 is an orally active antibacterial peptide. Protegrin-1 activates ERK, COX2, NFκB, inhibits Apoptosis, and NO production. Protegrin-1 has antibacterial activity against S. aureus, E. faecium, E. coli, P. aeruginosa and K. Pneumoniae, with MBC values between 10 and 20 µM. Protegrin-1 has antiviral activity against dengue NS2B-NS3. Protegrin-1 has anti-inflammatory activity. Protegrin-1 is used in the study of inflammatory diseases and infections^{[1][2][3][4][5][6][7][8]}.

Protegrin-1 (2.5-12.5 μM; 24-72  h) inhibits dengue NS2B-NS3 serine protease and viral replication in MK2 cells^[1].
Protegrin-1 (1-9 μM; 16 h) promotes the migration of IPEC-J2 cells^[2].
Protegrin-1 (>100 μM; 24 h) reduces the viability of 661W and PMN cells^[3].
Protegrin-1 (0.1-10 μg/mL; 24 h) inhibits porcine ovarian granulosa cell apoptosis from Hydrogen peroxide-induced oxidative stress via the PERK/eIF2a/CHOP signaling pathway^[5].
Protegrin-1 shows antimicrobial activity against S. aureus, E. faecium, E. coli, P. aeruginosa and K. Pneumoniae, with MBC values between 10 and 20 µM^[6].
Protegrin-1 (1.25-20 μM) inhibits LPS-induced activation of RAW macrophages, inhibiting the NO production^[6].

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

Protegrin-1 (0.5 mg/kg; i.p.; single) reduces the mortality of immunocompetent mice inoculated intraperitoneally with Pseudomonas aeruginosa or Staphylococcus aureus^[7].
Protegrin-1 (5 mg/kg; i.v.; single) reduces the mortality of mice inoculated intravenously with Staphylococcus aureus^[7].
Protegrin-1 (10 mg/kg; p.o.) reduces Citrobacter rodentium intestinal infection in mice as evidenced by reduced histopathologic change in the colon, prevention of body weight loss, milder clinical signs of disease^[8].

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

2155.61

C₈₈H₁₄₇N₃₇O₁₉S₄

168831-77-4

Solid

White to off-white

Arg-Gly-Gly-Arg-Leu-Cys-Tyr-Cys-Arg-Arg-Arg-Phe-Cys-Val-Cys-Val-Gly-Arg-NH2 (Disulfide bridge:Cys6-Cys15;Cys8-Cys13)

RGGRLCYCRRRFCVCVGR-NH2 (Disulfide bridge:Cys6-Cys15;Cys8-Cys13)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Rothan HA, et al. Protegrin-1 inhibits dengue NS2B-NS3 serine protease and viral replication in MK2 cells. J Biomed Biotechnol. 2012;2012:251482.  [Content Brief]

  [2]. Penney J, et al. Protegrin 1 Enhances Innate Cellular Defense via the Insulin-Like Growth Factor 1 Receptor Pathway. Front Cell Infect Microbiol. 2018 Sep 28;8:331.  [Content Brief]

  [3]. Soundrarajan N, et al. Protegrin-1 cytotoxicity towards mammalian cells positively correlates with the magnitude of conformational changes of the unfolded form upon cell interaction. Sci Rep. 2019 Aug 9;9(1):11569.  [Content Brief]

  [4]. Tu Y, et al. Effect of astragalus and astragalus polysaccharide on antimicrobial peptides PR-39 and protegrin-1 gene expression in pigs. Turkish Journal of Veterinary & Animal Sciences, 2006, 30(3): 325-330.

  [5]. Li X, et al. Protegrin-1 inhibits porcine ovarian granulosa cell apoptosis from H2O2-induced oxidative stress via the PERK/eIF2α/CHOP signaling pathway in vitro. Theriogenology. 2022 Feb;179:117-127.  [Content Brief]

  [6]. Javed A, et al. Antimicrobial and immunomodulatory activities of porcine cathelicidin Protegrin-1. Mol Immunol. 2024 Sep;173:100-109.  [Content Brief]

  [7]. Steinberg DA, et al. Protegrin-1: a broad-spectrum, rapidly microbicidal peptide with in vivo activity. Antimicrob Agents Chemother. 1997 Aug;41(8):1738-42.  [Content Brief]

  [8]. Osakowicz C, et al. Protective and Anti-Inflammatory Effects of Protegrin-1 on Citrobacter rodentium Intestinal Infection in Mice. Int J Mol Sci. 2021 Aug 31;22(17):9494.  [Content Brief]