PPACK dihydrochloride - CAS:82188-90-7

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PPACK dihydrochloride

目录号 : KM32655 CAS No. : 82188-90-7 纯度 : 99%

Data Sheet 产品使用指南

PPACK dihydrochloride 是一种靶向凝血酶 (thrombin) 和颗粒酶 GZMK 的高效、肽类抑制剂。PPACK dihydrochloride 特异性阻断 thrombin 和 GZMK 的活性，从而抑制凝血酶介导的 PAR-1 切割、下游炎症及促凝血信号通路。PPACK dihydrochloride 通过稳定 IκB 蛋白、阻断 NF-κB 活化及降低全身促炎/促凝血标志物水平，展现抗炎、抗血栓、屏障修复及抑制动脉粥样硬化斑块进展等多重作用。PPACK dihydrochloride 能在不受激肽原干扰的情况下结合血小板，有效限制急性血栓生长并减少哮喘模型中的嗜酸粒细胞浸润与杯状细胞增生。PPACK dihydrochloride 是研究动脉粥样硬化、哮喘及相关血栓炎症性疾病机制的重要工具分子。

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock

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Other Forms of Rapamycin:

PPACK dihydrochloride In-stock
PPACK TFA In-stock
AY 77 In-stock
CV-6209 (chloride) In-stock
RWJ-56110 dihydrochloride In-stock

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生物活性

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

IC₅₀&Target

PAR1

体外研究

PPACK dihydrochloride nanoparticles can completely inhibit thrombin-induced PAR-1 receptor cleavage on human aortic endothelial cells and tissue factor expression on THP-1 monocyte surfaces.
PPACK dihydrochloride nanoparticles can inhibit thrombin-induced NF-κB activation in human aortic endothelial cells and THP-1 monocytes.
PPACK dihydrochloride (5-fold molar excess; room temperature; 1 h) can inactivate the amide hydrolytic activity of human α-thrombin upon incubation at room temperature for 1 h, generating PPACK dihydrochloride-thrombin that does not interfere with the enzymatic function of unmodified α-thrombin.
PPACK dihydrochloride (200 μM, 100 μM, 10 μM) exhibits anticoagulant effects and demonstrates stronger anticoagulant activity at the same molar concentration compared to the factor Xa inhibitor GGACK when used alone.

Immunofluorescence

Cell Line:	Human aortic endothelial cells and THP-1 monocytes
Concentration:	PPACK nanoparticle
Incubation Time:	6 hours
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.

体内研究

PPACK dihydrochloride nanoparticles (intravenous injection; three times a week; lasting for four weeks) can reduce the blood vessel procoagulant activity, restore the integrity of endothelial barrier, delay the progress of plaque and weaken the inflammatory signal transduction in atherosclerotic plaque, without inducing systemic anticoagulation or changing serum cholesterol level.
PPACK (62.5 μg; i.p.; once every 2 days); Injecting dihydrochloride within 8-18 days after immunization can significantly alleviate airway eosinophilia, goblet cell proliferation, and airway hyperresponsiveness in a mouse model of asthma.

Animal Model:	C57BL/6J mice with Asthma (sex- and age-matched)
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.

分子式

C₂₁H₃₃Cl₃N₆O₃

分子量

523.88

CAS号

82188-90-7

中文名称

化合物 Ppack HCl

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, Sealed storage, away from moisture

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL (190.88 mM; Need ultrasonic)

H2O : 50 mg/mL (95.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9088 mL	9.5442 mL	19.0883 mL
5 mM	0.3818 mL	1.9088 mL	3.8177 mL
10 mM	0.1909 mL	0.9544 mL	1.9088 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： 99%

Data Sheet

产品使用指南

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.

Lan F, et al. GZMK-expressing CD8⁺ T cells promote recurrent airway inflammatory diseases. Nature. 2025;638(8050):490-498.

Schmaier AH, et al. PPACK-thrombin is a noncompetitive inhibitor of alpha-thrombin binding to human platelets. Thromb Res. 1992;67(5):479-489.

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.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器