PAI-1
Based on 1 Customer Validation
PAI-1 is a serine protease inhibitor (SERPIN). PAI-1 binds to and irreversibly inhibits uPA, tPA and furin; it also interacts with vitronectin, α1-acid glycoprotein, CRT, TLR4, proteasome α-3 subunit, uPAR, LRP1, Integrin αvβ3 and thrombin. PAI-1 regulates fibrinolysis, extracellular matrix turnover, cell migration, angiogenesis, inflammatory response and tissue remodeling; it mediates epithelial-mesenchymal transition (EMT)/endothelial-mesenchymal transition (EndMT), apoptosis and thrombus stabilization. PAI-1 can be used in research related to sepsis, acute lung injury, cardiovascular diseases, tissue fibrosis, diabetic nephropathy, obstructive nephropathy and non-insulin-dependent diabetes mellitus.
For research use only. We do not sell to patients.
- Purity : 98.55%
- CAS No.: 139446-70-1
- Formula: C27H47N9O9S
- Molecular Weight:673.78
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Storage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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uPA |
TPa |
uPAR |
LRP1 |
αvβ3 |
TLR4 |
CRT |
In Vitro
Rabbit anti-PAI-1 antibodies (1 μg/mL; 90 min) significantly enhance phagocytosis of viable wild-type mouse bone marrow neutrophils by mouse peritoneal macrophages, a PAI-1-dependent effect[1].
Mouse recombinant PAI-1 (1 μg/mL; 90 min) inhibits the enhanced phagocytosis of viable wild-type mouse bone marrow neutrophils by mouse peritoneal macrophages induced by CD47 blockade[1].
Mouse recombinant PAI-1 (1 μg/mL) reduces elevated surface calreticulin levels on viable PAI-1-/- mouse bone marrow neutrophils to wild-type levels[1].
PAI-1 controls collagen levels, a key profibrotic marker, in human keloid-derived skin fibroblasts, with overexpression increasing collagen accumulation and depletion reducing it[3].
PAI-1 (5 μg; 2 h at 4°C) and Guanidine hydrochloride (HY-B0178A)-activated PAI-1 (4 M; 2 h at 20°C pre-treatment) bind to Heparin (HY-17567)-Sepharose at pH 7.4, with non-activated PAI-1 exhibiting a sharper elution profile at higher Na+Cl− concentrations than activated PAI-1[5].
PAI-1 has binding to heparin-Sepharose competed by soluble heparin and low molecular weight heparin, with soluble heparin exhibiting ~10-fold higher affinity for PAI-1 than low molecular weight heparin, as indicated by IC50 values of 7.0 μM and 73 μM, respectively[5].
PAI-1 (5 nM; 1 h at 37°C) has heparin dose-dependently mediate inhibition of α-thrombin, with maximal inhibition at 1 unit/mL heparin and a corresponding second-order association rate constant of 1.0 × 105 M-1s-1[5].
PAI-1 (7 nM; 1 h at 37°C) has heparin dose-dependently promote the formation of SDS-stable complexes with human α-thrombin, with maximal complex formation occurring at 1 unit/mL heparin[5].
PAI-1 potently inhibits the enzymatic activity of free tPA, reducing its activity by 82% when used at equivalent molar amounts[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8-10-week-old, age- and sex-matched)[1]
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Dosage:2 μg per injection
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Administration:intratracheal; preincubation with neutrophils prior to administration
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Result:Significantly reduced phagocytic index (percentage of alveolar macrophages containing at least one ingested neutrophil) compared to mouse albumin control (P < 0.01).
- Collagen: Sirius Red Staining
- Human pluripotent stem cell endothelial-cell differentiation
- Cell migration
- ECM-Embedded Organoid (Matrigel/Dome) Culture
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Research Protocol for Endocrine Diseases
- Transwell/Boyden Chamber Migration Assay
- Endothelial Tube Formation Assay
- 3D Collagen/Hydrogel Matrix Migration Assay
- Apoptosis Solutions
- Matrigel/ECM Transwell Invasion Assay
- Inhalation Toxicity Study
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Scratch/Wound-Healing Migration Assay
- Vascular/Branching Fractal Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- Neural Crest/Neuronal Cell Migration Explant Assay
- Research Protocol for Inflammation-related Diseases
- Research Protocol for Metabolic Diseases
- Matrigel Transwell/Boyden Chamber Invasion Assay
- Fibrosis/Collagen Morphometry
- LPS-Induced Endotoxemia/Systemic Inflammation
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 139446-70-1
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Appearance Solid
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Molecular Weight 673.78
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Formula C27H47N9O9S
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Sequence
Ala-Arg-Met-Ala-Pro-Glu
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Sequence Shortening
ARMAPE
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (148.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
[1]. Park YJ, et al. PAI-1 inhibits neutrophil efferocytosis. Proceedings of the National Academy of Sciences of the United States of America. 2008 Aug 19;105(33):11784-9. [Content Brief]
[2]. Sillen M, et al. Targeting PAI-1 in Cardiovascular Disease: Structural Insights Into PAI-1 Functionality and Inhibition. Frontiers in cardiovascular medicine. 2020;7:622473. [Content Brief]
[3]. Ghosh AK, et al. PAI-1 in tissue fibrosis. Journal of cellular physiology. 2012 Feb;227(2):493-507. [Content Brief]
[4]. Huang Y, Border WA, Yu L, Zhang J, Lawrence DA, Noble NA. A PAI-1 mutant, PAI-1R, slows progression of diabetic nephropathy. J Am Soc Nephrol. 2008 Feb;19(2):329-38. [Content Brief]
[5]. Ehrlich HJ, et al. Functional interaction of plasminogen activator inhibitor type 1 (PAI-1) and heparin. Biochemistry. 1991 Jan 29;30(4):1021-8. [Content Brief]
[6]. Oda T, et al. PAI-1 deficiency attenuates the fibrogenic response to ureteral obstruction. Kidney international. 2001 Aug;60(2):587-96. [Content Brief]
[7]. Matsuo S, et al. Multifunctionality of PAI-1 in fibrogenesis: evidence from obstructive nephropathy in PAI-1-overexpressing mice. Kidney Int. 2005 Jun;67(6):2221-38. [Content Brief]
[8]. Vaughan DE. PAI-1 and atherothrombosis. J Thromb Haemost. 2005 Aug;3(8):1879-83. [Content Brief]
[9]. Tang Z, et al. Surface immobilization of a protease through an inhibitor-derived affinity ligand: a bioactive surface with defensive properties against an inhibitor. Chemical communications (Cambridge, England). 2015 Sep 28;51(75):14263-6. [Content Brief]
[10]. Nordt TK, et al. Induction of plasminogen activator inhibitor type-1 (PAI-1) by proinsulin and insulin in vivo. Circulation. 1995 Feb 01;91(3):764-70. [Content Brief]
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 and light). 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 |
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| DMSO | 1 mM | 1.4842 mL | 7.4208 mL | 14.8416 mL | 37.1041 mL |
| 5 mM | 0.2968 mL | 1.4842 mL | 2.9683 mL | 7.4208 mL | |
| 10 mM | 0.1484 mL | 0.7421 mL | 1.4842 mL | 3.7104 mL | |
| 15 mM | 0.0989 mL | 0.4947 mL | 0.9894 mL | 2.4736 mL | |
| 20 mM | 0.0742 mL | 0.3710 mL | 0.7421 mL | 1.8552 mL | |
| 25 mM | 0.0594 mL | 0.2968 mL | 0.5937 mL | 1.4842 mL | |
| 30 mM | 0.0495 mL | 0.2474 mL | 0.4947 mL | 1.2368 mL | |
| 40 mM | 0.0371 mL | 0.1855 mL | 0.3710 mL | 0.9276 mL | |
| 50 mM | 0.0297 mL | 0.1484 mL | 0.2968 mL | 0.7421 mL | |
| 60 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.6184 mL | |
| 80 mM | 0.0186 mL | 0.0928 mL | 0.1855 mL | 0.4638 mL | |
| 100 mM | 0.0148 mL | 0.0742 mL | 0.1484 mL | 0.3710 mL |
PAI-1 Related Classifications
HY-P11413 Related Classifications
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