PXS-4787
PXS-4787 is a specific and effective pan-LOX (lysyl oxidase) inhibitor for abolishing lysyl oxidase activity. PXS-4787 inhibits LOX with IC50s of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4), respectively.
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- CAS. Nr.: 2409963-50-2
- Formel: C10H12FNO2S
- Molecular Weight:229.27
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4)[1]
Lysyl oxidases stabilize the main component of scar tissue, collagen, and drive scar stiffness and appearance[1].
PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species[1].
PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro[1].
PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary human dermal fibroblasts cultured in vitro
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Concentration:0, 1, 10 μM
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Incubation Time:11 days
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Result:Significantly reduced in the 10 µM treatment group.
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Cell Line:Cultured fibroblasts and keratinocytes (isolated from five different patients)
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Concentration:10 μM
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Incubation Time:48 hours
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Result:Resulted four genes with significant differential expression in fibroblasts and two differentially expressed genes in keratinocytes.
PXS-4787 (3%, oil in water cream; 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: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 dailly, for 12 weeks
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Result:Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect.
Chemical Information
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CAS. Nr. 2409963-50-2
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Molecular Weight 229.27
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Formel C10H12FNO2S
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SMILES
NC/C=C(CS(=O)(C1=CC=CC=C1)=O)\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
DMSO : 25 mg/mL (109.04 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3617 mL | 21.8083 mL | 43.6167 mL | 109.0417 mL |
| 5 mM | 0.8723 mL | 4.3617 mL | 8.7233 mL | 21.8083 mL | |
| 10 mM | 0.4362 mL | 2.1808 mL | 4.3617 mL | 10.9042 mL | |
| 15 mM | 0.2908 mL | 1.4539 mL | 2.9078 mL | 7.2694 mL | |
| 20 mM | 0.2181 mL | 1.0904 mL | 2.1808 mL | 5.4521 mL | |
| 25 mM | 0.1745 mL | 0.8723 mL | 1.7447 mL | 4.3617 mL | |
| 30 mM | 0.1454 mL | 0.7269 mL | 1.4539 mL | 3.6347 mL | |
| 40 mM | 0.1090 mL | 0.5452 mL | 1.0904 mL | 2.7260 mL | |
| 50 mM | 0.0872 mL | 0.4362 mL | 0.8723 mL | 2.1808 mL | |
| 60 mM | 0.0727 mL | 0.3635 mL | 0.7269 mL | 1.8174 mL | |
| 80 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3630 mL | |
| 100 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0904 mL |
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