PXS-5120A
Based on 1 Customer Validation
PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).
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- Reinheit: 98.12%
- CAS. Nr.: 2125955-70-4
- Formel: C22H25ClFN3O4S
- Molecular Weight:481.97
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like); Ki: 83 nM (Lysyl Oxidase-like 2)[1]
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
16 nM
Compound: 12k; PXS-5120A
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Inhibition of recombinant C-terminal His-tagged human LOXL3 (1 to 753 residues) expressed in CHO cells using putrescine as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured every 2.5 mins for 30 mins by Amplex-Red
Inhibition of recombinant C-terminal His-tagged human LOXL3 (1 to 753 residues) expressed in CHO cells using putrescine as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured every 2.5 mins for 30 mins by Amplex-Red
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[PMID: 31580073] |
PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4 with IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2125955-70-4
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Appearance Solid
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Molecular Weight 481.97
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Formel C22H25ClFN3O4S
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Color White to off-white
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SMILES
O=C(C1=CC2=C(N(C/C(F)=C/CN)C(C)=C2C3=CC=CC(S(=O)(N(C)C)=O)=C3)C=C1)O.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (259.35 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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). 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 | 2.0748 mL | 10.3741 mL | 20.7482 mL | 51.8704 mL |
| 5 mM | 0.4150 mL | 2.0748 mL | 4.1496 mL | 10.3741 mL | |
| 10 mM | 0.2075 mL | 1.0374 mL | 2.0748 mL | 5.1870 mL | |
| 15 mM | 0.1383 mL | 0.6916 mL | 1.3832 mL | 3.4580 mL | |
| 20 mM | 0.1037 mL | 0.5187 mL | 1.0374 mL | 2.5935 mL | |
| 25 mM | 0.0830 mL | 0.4150 mL | 0.8299 mL | 2.0748 mL | |
| 30 mM | 0.0692 mL | 0.3458 mL | 0.6916 mL | 1.7290 mL | |
| 40 mM | 0.0519 mL | 0.2594 mL | 0.5187 mL | 1.2968 mL | |
| 50 mM | 0.0415 mL | 0.2075 mL | 0.4150 mL | 1.0374 mL | |
| 60 mM | 0.0346 mL | 0.1729 mL | 0.3458 mL | 0.8645 mL | |
| 80 mM | 0.0259 mL | 0.1297 mL | 0.2594 mL | 0.6484 mL | |
| 100 mM | 0.0207 mL | 0.1037 mL | 0.2075 mL | 0.5187 mL |
PXS-5120A Related Classifications
HY-130242 Related Classifications
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