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)
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
Ki: 37 nM (SSAO)[1]
In Vitro
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. Further protocols information, click here.
In Vivo
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
In Vitro:
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)
Protokoll
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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 |
PXS-4681A Related Classifications
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