PXS-4681A
Based on 1 Customer Validation
PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.40%
- CAS. Nr.: 1478364-87-2
- Formel: C10H14ClFN2O3S
- Molecular Weight:296.75
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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)
Biologische Aktivität
Ki: 37 nM (SSAO)[1]
PXS-4681A is an inhibitor of SSAO/VAP-1 in human, rat, mouse, rabbit, and dog species with IC50 values of 3 nM, 3 nM, 2 nM, 9 nM and 3nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In rats, PXS-4681A is well absorbed with good bioavailability and oral half-life at the 10 mg/kg i.v. dose and the 20 mg/kg PO dose. Similarly, in BALB/C mice, PXS-4681A is well absorbed with good bioavailability and oral half-life at 2 mg/kg in both intravenous and oral studies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Carrageenan-induced skin inflammation mice[1]
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Dosage:2 mg/kg
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Administration:oral administration; single dose
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Result:Reduced local inflammation, causing a significant reduction in exudate volume by 25%.
Chemical Information
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CAS. Nr. 1478364-87-2
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Appearance Solid
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Molecular Weight 296.75
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Formel C10H14ClFN2O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(OC/C(CN)=C\F)C=C1)(N)=O.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 : 250 mg/mL (842.46 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 (273 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3698 mL | 16.8492 mL | 33.6984 mL | 84.2460 mL |
| 5 mM | 0.6740 mL | 3.3698 mL | 6.7397 mL | 16.8492 mL | |
| 10 mM | 0.3370 mL | 1.6849 mL | 3.3698 mL | 8.4246 mL | |
| 15 mM | 0.2247 mL | 1.1233 mL | 2.2466 mL | 5.6164 mL | |
| 20 mM | 0.1685 mL | 0.8425 mL | 1.6849 mL | 4.2123 mL | |
| 25 mM | 0.1348 mL | 0.6740 mL | 1.3479 mL | 3.3698 mL | |
| 30 mM | 0.1123 mL | 0.5616 mL | 1.1233 mL | 2.8082 mL | |
| 40 mM | 0.0842 mL | 0.4212 mL | 0.8425 mL | 2.1061 mL | |
| 50 mM | 0.0674 mL | 0.3370 mL | 0.6740 mL | 1.6849 mL | |
| 60 mM | 0.0562 mL | 0.2808 mL | 0.5616 mL | 1.4041 mL | |
| 80 mM | 0.0421 mL | 0.2106 mL | 0.4212 mL | 1.0531 mL | |
| 100 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8425 mL |