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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 2409963-50-2
- 화학식: C10H12FNO2S
- 분자량:229.27
-
보관:
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]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
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.
-
Cell Line:Primary human dermal fibroblasts cultured in vitro
-
Concentration:0, 1, 10 μM
-
Incubation Time:11 days
-
Result:Significantly reduced in the 10 µM treatment group.
-
Cell Line:Cultured fibroblasts and keratinocytes (isolated from five different patients)
-
Concentration:10 μM
-
Incubation Time:48 hours
-
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.
-
Animal Model:Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1]
-
Dosage:3%, oil in water cream; 400 mg cream applied to 16 cm2
-
Administration:External application; 1, 2 and 3 weeks post-injury; once dailly, for 12 weeks
-
Result:Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect.
Chemical Information
-
CAS No. 2409963-50-2
-
분자량 229.27
-
화학식 C10H12FNO2S
-
SMILES
NC/C=C(CS(=O)(C1=CC=CC=C1)=O)\F
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
References
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 |
PXS-4787 Related Classifications
HY-151498 Related Classifications
Powered by Bioz