PXS-6302
PXS-6302 is an irreversible lysyl oxidase inhibitor with IC50s of 3.7 μM (Bovine LOX), 3.4 μM (rh LOXL1), 0.4 μM (rh LOXL2), 1.5 μM (rh LOXL3), 0.3 μM (rh LOXL4), respectively. PXS-6302 has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance.
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- CAS. Nr.: 2584947-54-4
- Formel: C10H10F3NO2S
- Molecular Weight:265.25
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
3.7 μM (Bovine LOX), 3.4 μM (rh LOXL1), 0.4 μM (rh LOXL2), 1.5 μM (rh LOXL3), 0.3 μM (rh LOXL4)[1]
In Vitro
PXS-6302 demonstrates high permeability to across a monolayer of cells, such as Caco-2 or MDCKII cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
PXS-6302 (1.5%, oil in water cream; 500 mg cream applied to 16 cm2; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in murine models of injury and fibrosis under topical application[1].
PXS-6302 (0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm2; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1]
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Dosage:0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm2
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Administration:External application; 1, 2 and 3 weeks post-injury; once dayly, for 12 weeks
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Result:Showed significantly higher scores for the 3% treated scars suggesting significant improvement in scar appearance.
Chemical Information
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CAS. Nr. 2584947-54-4
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Molecular Weight 265.25
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Formel C10H10F3NO2S
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SMILES
NC/C=C(C(F)(S(=O)(C1=CC=CC=C1)=O)F)\F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (377.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.43 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Protokoll
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7700 mL | 18.8501 mL | 37.7003 mL | 94.2507 mL |
| 5 mM | 0.7540 mL | 3.7700 mL | 7.5401 mL | 18.8501 mL | |
| 10 mM | 0.3770 mL | 1.8850 mL | 3.7700 mL | 9.4251 mL | |
| 15 mM | 0.2513 mL | 1.2567 mL | 2.5134 mL | 6.2834 mL | |
| 20 mM | 0.1885 mL | 0.9425 mL | 1.8850 mL | 4.7125 mL | |
| 25 mM | 0.1508 mL | 0.7540 mL | 1.5080 mL | 3.7700 mL | |
| 30 mM | 0.1257 mL | 0.6283 mL | 1.2567 mL | 3.1417 mL | |
| 40 mM | 0.0943 mL | 0.4713 mL | 0.9425 mL | 2.3563 mL | |
| 50 mM | 0.0754 mL | 0.3770 mL | 0.7540 mL | 1.8850 mL | |
| 60 mM | 0.0628 mL | 0.3142 mL | 0.6283 mL | 1.5708 mL | |
| 80 mM | 0.0471 mL | 0.2356 mL | 0.4713 mL | 1.1781 mL | |
| 100 mM | 0.0377 mL | 0.1885 mL | 0.3770 mL | 0.9425 mL |
PXS-6302 Related Classifications
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