PPACK
Based on 4 publication(s) in Google Scholar
PPACK is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.
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- No. CAS: 71142-71-7
- Fòrmula: C21H31ClN6O3
- Peso molecular:450.96
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) PPACK
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Flow Cytometry
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Cell Imaging/Staining
Actividad biológica
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PAR1 |
PPACK nanoparticles completely inhibit thrombin-induced cleavage of the PAR-1 receptor on human aortic endothelial cells, as well as tissue factor expression on the surface of THP-1 monocytes[1].
PPACK nanoparticles inhibit thrombin-induced NF-κB activation in human aortic endothelial cells and THP-1 monocytes[1].
PPACK (5-fold molar excess; room temperature; 1 h) inactivates the amidolytic activity of human α-thrombin after 1 h of incubation at room temperature, generating PPACK-thrombin that does not interfere with the enzymatic function of unmodified α-thrombin[4].
PPACK (200 μM, 100 μM, 10 μM) exerts anticoagulant effects, and exhibits stronger anticoagulant activity on a molar basis than the factor Xa inhibitor GGACK (HY-137495) used alone at the same concentrations[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human aortic endothelial cells and THP-1 monocytes
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Concentration:PPACK nanoparticle
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Incubation Time:6 h
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Result:Inhibited thrombin-induced NF-κB activation in human aortic endothelial cells and THP-1 monocytes.
Resulted in little to no observable posi- tive staining for intracellular phospho-p65 and preservation of IkB protein.
PPACK (62.5 μg; i.p.; every 2 days; 8 to 18 days post-immunization) significantly attenuates airway eosinophilia, goblet cell hyperplasia and airway hyperresponsiveness in a mouse model of asthma[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice with Asthma (sex- and age-matched)[3]
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Dosage:62.5 μg
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Administration:i.p.; every 2 days; 8 to 18 days post-immunization
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Result:Significantly reduced eosinophil counts in bronchoalveolar lavage fluid (BALF).\nSignificantly reduced goblet cell hyperplasia in lung tissue.\nSignificantly improved lung function via reduced airway resistance in response to methacholine challenge.
Chemical Information
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No. CAS 71142-71-7
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Peso molecular 450.96
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Fòrmula C21H31ClN6O3
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Sequence
{d-Phe}-Pro-{Arg-Chloromethylketone}
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Sequence Shortening
{d-Phe}-P-{Arg-Chloromethylketone}
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Nature
2025 Feb;638(8050):490-498. PMID: 39814882
PPACK purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):490-498. [Abstract]
Summary statistics showing the number of different immune cells in the BALF of PPACK (PPACK TFA) (62.5 μg per mouse; i.p.; every 2 days) treated mice. Each symbol indicates one mouse, and lines denote means.
PPACK purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):490-498. [Abstract]
Airway hypersensitivity of the vehicle or PPACK (PPACK TFA) (62.5 μg per mouse; i.p.; every 2 days) treated mice measured using the forced oscillation technique. Each symbol indicates one mouse, and bars denote means.
PPACK purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):490-498. [Abstract]
Representative AB-PAS staining of lung tissue sections of vehicle or PPACK (PPACK TFA) (62.5 μg per mouse; i.p.; every 2 days) treated mice. Scale bar, 100 μm. Statistics summarizing the PAS+ areas in the airway of indicated mice. Each symbol indicates one mouse, and lines denote means.
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J Thromb Thrombolysis
The inhibitory effect of antiplatelet drugs on spontaneous platelet aggregation on glass surfaces: an analysis based on microscopic three-dimensional topography. [Abstract]2025 Sep 9. PMID: 40924280
PPACK purchased from MedChemExpress. Usage Cited in: J Thromb Thrombolysis. 2025 Sep 9. [Abstract]
PPACK (PPACK TFA)-anticoagulated PRP droplets deposited on the glass surface. The results showed that 100 μM PPACK-anticoag-ulated PRP on the glass surface retained the ability to form platelet aggregates on the glass surface.
Pureza y Documentación
Referencias
[1]. Palekar RU, et al. Inhibition of Thrombin With PPACK-Nanoparticles Restores Disrupted Endothelial Barriers and Attenuates Thrombotic Risk in Experimental Atherosclerosis. Arterioscler Thromb Vasc Biol. 2016;36(3):446-455. [Content Brief]
[2]. Wu Y, et al. The inhibitory effect of antiplatelet drugs on spontaneous platelet aggregation on glass surfaces: an analysis based on microscopic three-dimensional topography. J Thromb Thrombolysis. Published online September 9, 2025. [Content Brief]
[3]. Lan F, et al. GZMK-expressing CD8+ T cells promote recurrent airway inflammatory diseases. Nature. 2025;638(8050):490-498. [Content Brief]
[4]. Schmaier AH, et al. PPACK-thrombin is a noncompetitive inhibitor of alpha-thrombin binding to human platelets. Thromb Res. 1992;67(5):479-489. [Content Brief]
[5]. Lyon ME, et al. Evaluation of the thrombin inhibitor D-phenylalanyl-L-prolyl-L-arginine chloromethylketone (PPACK) with the factor Xa inhibitor 1,5-dansyl-L-glutamyl-L-glycyl-L-arginine chloromethylketone (GGACK) as anticoagulants for critical care clinical chemistry specimens. Clin Chim Acta. 1999 Feb;280(1-2):91-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PPACK Related Classifications
HY-122542 Related Classifications
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