製品番号: HY-122542B

PPACK TFA

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

PPACK TFA is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK TFA 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 TFA exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK TFA binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK TFA is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 96.79%
CAS 番号: 157379-44-7
分子式: C₂₃H₃₂ClF₃N₆O₅
分子量:564.99

保管条件:

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)

PPACK TFA 構造式

CAS 番号: 157379-44-7

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

MedChemExpress（MCE）の使用を引用している文献 PPACK TFA

Customer Validation & Images

Cell Imaging/StainingFlow CytometryIn Vivo Efficacy StudyHistological Imaging/Staining

Flow Cytometry
In Vivo Efficacy Study
Histological Imaging/Staining
Cell Imaging/Staining

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (2)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

PAR1

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

体外実験

PPACK TFA 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 TFA nanoparticles inhibit thrombin-induced NF-κB activation in human aortic endothelial cells and THP-1 monocytes^[1].
PPACK TFA (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 TFA-thrombin that does not interfere with the enzymatic function of unmodified α-thrombin^[4].
PPACK TFA (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.

Immunofluorescence^[1]

Cell Line:

Human aortic endothelial cells and THP-1 monocytes
Concentration:

PPACK nanoparticle
Incubation Time:

6 h
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.

体内実験

Intravenous administration of PPACK TFA nanoparticles (intravenous injection; 3 times per week; for 4 consecutive weeks) to high-fat diet-fed ApoE knockout mice reduces vascular procoagulant activity, restores endothelial barrier integrity, delays plaque progression, and attenuates inflammatory signaling in atherosclerotic plaques, without inducing systemic anticoagulation or altering serum cholesterol levels^[1].
PPACK (62.5 μg; i.p.; every 2 days; 8 to 18 days post-immunization) TFA 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.

Animal Model:

C57BL/6J mice with Asthma (sex- and age-matched)^[3]
Dosage:

62.5 μg
Administration:

i.p.; every 2 days; 8 to 18 days post-immunization
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.

化学情報

CAS 番号 157379-44-7
性状 Solid
分子量 564.99
分子式 C₂₃H₃₂ClF₃N₆O₅
Color White to off-white
SMILES

O=C([C@H]1N(CCC1)C([C@H](N)CC2=CC=CC=C2)=O)N[C@@H](CCCNC(N)=N)C(CCl)=O.O=C(C(F)(F)F)O
配列

{d-Phe}-Pro-{Arg-Chloromethylketone}
シーケンスの短縮

{d-Phe}-P-{Arg-Chloromethylketone}
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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)

Publications (2)

All Cell Imaging/StainingFlow CytometryIn Vivo Efficacy StudyHistological Imaging/Staining

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Journal Impact Factor

Nature

GZMK-expressing CD8+ T cells promote recurrent airway inflammatory diseases. [Abstract]

2025 Feb;638(8050):490-498. PMID: 39814882

PPACK TFA 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 TFA 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 TFA 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.
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 TFA 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.

溶剤 & 溶解度

体外:

DMSO : 250 mg/mL (442.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7699 mL

8.8497 mL

17.6994 mL

5 mM

0.3540 mL

1.7699 mL

3.5399 mL

10 mM

0.1770 mL

0.8850 mL

1.7699 mL

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (287 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7699 mL	8.8497 mL	17.6994 mL	44.2486 mL
	5 mM	0.3540 mL	1.7699 mL	3.5399 mL	8.8497 mL
	10 mM	0.1770 mL	0.8850 mL	1.7699 mL	4.4249 mL
	15 mM	0.1180 mL	0.5900 mL	1.1800 mL	2.9499 mL
	20 mM	0.0885 mL	0.4425 mL	0.8850 mL	2.2124 mL
	25 mM	0.0708 mL	0.3540 mL	0.7080 mL	1.7699 mL
	30 mM	0.0590 mL	0.2950 mL	0.5900 mL	1.4750 mL
	40 mM	0.0442 mL	0.2212 mL	0.4425 mL	1.1062 mL
	50 mM	0.0354 mL	0.1770 mL	0.3540 mL	0.8850 mL
	60 mM	0.0295 mL	0.1475 mL	0.2950 mL	0.7375 mL
	80 mM	0.0221 mL	0.1106 mL	0.2212 mL	0.5531 mL
	100 mM	0.0177 mL	0.0885 mL	0.1770 mL	0.4425 mL

Keywords

PPACK TFA

2 Cited Publications

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PPACK TFA

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

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MedChemExpress（MCE）の使用を引用している文献 PPACK TFA

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PPACK TFA 関連分類

HY-122542B 関連分類