1. GPCR/G Protein Immunology/Inflammation Apoptosis
  2. CXCR Apoptosis IFNAR TNF Receptor Interleukin Related
  3. Ac-Pro-Gly-Pro-OH

Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and acts as a CXCR2 agonist. Ac-Pro-Gly-Pro-OH exerts bactericidal activity by generating hydrogen peroxide, inhibits pulmonary inflammation, and reduces immune cell apoptosis (apoptosis). Ac-Pro-Gly-Pro-OH promotes the production of IFN-γ and inhibits the production of TNF-α and IL-6 in leukocytes. Ac-Pro-Gly-Pro-OH increases the survival rate of mice in sepsis models, enhances the bactericidal activity of neutrophils, acts as a neutrophil chemoattractant, induces neutrophil polarization, and regulates inflammatory and repair processes. Ac-Pro-Gly-Pro-OH induces chronic inflammation and tissue remodeling through sustained action. Ac-Pro-Gly-Pro-OH is released via alkaline hydrolysis of corneal proteins in alkali-injured eyes, thereby driving the early infiltration of neutrophils into the cornea. Ac-Pro-Gly-Pro-OH is applicable to research related to sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcer.

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Custom Peptide Synthesis

Ac-Pro-Gly-Pro-OH

Ac-Pro-Gly-Pro-OH Chemical Structure

CAS No. : 292171-04-1

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Based on 2 publication(s) in Google Scholar

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Description

Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and acts as a CXCR2 agonist. Ac-Pro-Gly-Pro-OH exerts bactericidal activity by generating hydrogen peroxide, inhibits pulmonary inflammation, and reduces immune cell apoptosis (apoptosis). Ac-Pro-Gly-Pro-OH promotes the production of IFN-γ and inhibits the production of TNF-α and IL-6 in leukocytes. Ac-Pro-Gly-Pro-OH increases the survival rate of mice in sepsis models, enhances the bactericidal activity of neutrophils, acts as a neutrophil chemoattractant, induces neutrophil polarization, and regulates inflammatory and repair processes. Ac-Pro-Gly-Pro-OH induces chronic inflammation and tissue remodeling through sustained action. Ac-Pro-Gly-Pro-OH is released via alkaline hydrolysis of corneal proteins in alkali-injured eyes, thereby driving the early infiltration of neutrophils into the cornea. Ac-Pro-Gly-Pro-OH is applicable to research related to sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcer[1][2][3].

IC50 & Target[1]

CXCR2

 

In Vitro

Ac-Pro-Gly-Pro-OH (0-50 μM; 10 min) induces concentration-dependent hydrogen peroxide (H2O2) production in isolated mouse neutrophils via CXCR2[1].
Ac-Pro-Gly-Pro-OH (0-50 μM; 1 h) enhances the concentration-dependent bactericidal activity of isolated murine neutrophils[1].
Ac-Pro-Gly-Pro-OH (1-20 μM; 30 min pre-incubation, 24 h LPS stimulation) modulates cytokine production in LPS-stimulated mouse splenocytes, inhibits the pro-inflammatory cytokines TNF-α and IL-6 in a concentration-dependent manner, while enhancing the type 1 cytokine IFN-γ, with the most potent effect observed at 20 μM[1].
Ac-Pro-Gly-Pro-OH (0.1-50 μM; 1 h) enhances the concentration-dependent bactericidal activity of isolated human neutrophils, reaching a maximum killing rate (approximately 95%) at 20 μM and 50 μM[1].
Ac-Pro-Gly-Pro-OH (0-20 μM; 30 min pre-incubation, 3 h LPS stimulation) regulates cytokine production in LPS (HY-D1056)-stimulated human neutrophils and PBMCs. It inhibits the pro-inflammatory cytokine TNF-α and enhances the type 1 cytokine IFN-γ in a concentration-dependent manner, with the strongest effect observed at 20 μM[1].
Ac-Pro-Gly-Pro-OH activates neutrophils, mediates superoxide anion production, MMP-9 release and CXCL8 release by binding to CXCR1/2, and induces G protein-dependent neutrophil chemotaxis[2].
Ac-Pro-Gly-Pro-OH promotes CXCR2-dependent paracellular permeability in endothelial cells and the release of endothelin-1 in aortic endothelial cells[2].
Ac-Pro-Gly-Pro-OH induces CXCR2-dependent migration, proliferation and tube formation of endothelial progenitor cells[2].
Ac-Pro-Gly-Pro-OH resists degradation mediated by LTA4H, but is susceptible to degradation by ACE[2].
Ac-Pro-Gly-Pro-OH induces polarization in isolated human neutrophils with an EC50 of 0.50 mM[3].

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

ELISA Assay[1]

Cell Line: mouse splenocytes
Concentration: 1, 5, 10, and 20 μM
Incubation Time: 30 min pre-incubation, 3 h LPS stimulation
Result: Modulated cytokine production in LPS-stimulated mouse splenocytes, inhibited the pro-inflammatory cytokines TNF-α and IL-6 in a concentration-dependent manner, while enhancing the type 1 cytokine IFN-γ, with the most potent effect observed at 20 μM
In Vivo

Ac-Pro-Gly-Pro-OH (7.5-17.5 mg/kg; s.c.) significantly improves the survival rate of ICR mice with sepsis induced by CLP or E. coli in a dose-dependent manner by activating CXCR2, alleviates organ inflammation and immune cell apoptosis, enhances bacterial clearance, regulates cytokine production, and reduces the incidence of fatal sepsis in ICR mice with LPS-induced sepsis[1].
Ac-Pro-Gly-Pro-OH drives neutrophil recruitment and corneal ulcer formation in an alkali-injured rabbit corneal model[2].
Ac-Pro-Gly-Pro-OH induces dose-dependent airway neutrophilic inflammation in mice via the CXCR2 signaling pathway, triggers emphysema in *Mus musculus*, abrogates bleomycin hydrochloride (HY-17565A)-induced pulmonary fibrosis in mice, and promotes cutaneous neovascularization and wound healing in mice[2].

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

Animal Model: ICR (male, wild-type albino)[1]
Dosage: 7.5 mg/kg; 12.5 mg/kg; 17.5 mg/kg (survival, organ inflammation, bactericidal activity, cytokine modulation); 17.5 mg/kg (5 doses, survival); 17.5 mg/kg (delayed 4 doses, survival); 17.5 mg/kg (2 doses, organ inflammation)
Administration: s.c.; 4 doses at 2,14,26,38 hours post-CLP; 5 doses at 2,14,26,38,50 hours post-CLP; 4 doses at 10,22,34,48 hours post-CLP; 2 doses at 2,14 hours post-CLP/4 doses at 2,14,26,38 hours post-E. coli injection/4 doses at 2,14,26,38 hours post-LPS injection
Result: Increased survival in a dose-dependent manner.
Further improved survival when 17.5 mg/kg was given as 5 doses vs fewer doses.
Showed therapeutic effect on survival with delayed 17.5 mg/kg (4 doses starting 10 hours post-CLP).
Reduced CLP-induced acute lung injury score, thrombi and hyaline membrane score, and lung wet-to-dry weight ratio.
Inhibited CLP-induced liver inflammation, splenic and thymic tissue damage, and reduced TUNEL-positive cells in spleen and thymus by ~50-60% compared with vehicle controls.
Reduced intraperitoneal bacterial colony counts by 82.1% at 24 hours after CLP.
Blunted CLP-induced increases in peritoneal fluid TNF-α, IL-1β, and IL-6 levels, while enhancing production of type 1 cytokines IFN-γ, IL-12, and IL-2 in peritoneal fluid.
Reduced the incidence of fatal sepsis compared with vehicle controls.
Molecular Weight

311.33

Formula

C14H21N3O5

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Ac-Pro-Gly-Pro-OH

Sequence Shortening

Ac-PGP-OH

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (160.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2120 mL 16.0601 mL 32.1203 mL
5 mM 0.6424 mL 3.2120 mL 6.4241 mL
View the Complete Stock Solution Preparation Table

* 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.49%

References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.2120 mL 16.0601 mL 32.1203 mL 80.3006 mL
5 mM 0.6424 mL 3.2120 mL 6.4241 mL 16.0601 mL
10 mM 0.3212 mL 1.6060 mL 3.2120 mL 8.0301 mL
15 mM 0.2141 mL 1.0707 mL 2.1414 mL 5.3534 mL
20 mM 0.1606 mL 0.8030 mL 1.6060 mL 4.0150 mL
25 mM 0.1285 mL 0.6424 mL 1.2848 mL 3.2120 mL
30 mM 0.1071 mL 0.5353 mL 1.0707 mL 2.6767 mL
40 mM 0.0803 mL 0.4015 mL 0.8030 mL 2.0075 mL
50 mM 0.0642 mL 0.3212 mL 0.6424 mL 1.6060 mL
60 mM 0.0535 mL 0.2677 mL 0.5353 mL 1.3383 mL
80 mM 0.0402 mL 0.2008 mL 0.4015 mL 1.0038 mL
100 mM 0.0321 mL 0.1606 mL 0.3212 mL 0.8030 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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