CHF-6333 xinafoate
CHF-6333 xinafoate is a neutrophil elastase (NE) inhibitor (IC50 = 0.21 nM; KD = 0.16 nM). CHF6333 xinafoate retains its activity in both human (IC50 = 0.22 nM) and rat (IC50 = 3.63 nM) proteases. CHF6333 xinafoate exhibits inhibitory activity against Proteinase 3 (IC50 = 22 nM). CHF-6333 xinafoate can be used for the study of bronchiectasis (BE).
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- No. CAS: 3071964-44-5
- Fòrmula: C38H35F3N6O6
- Peso molecular:728.72
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
CHF6333 (Compound 15) (1 μM, 0-30 min) xinafoate exhibits a half-life (t1/2) greater than 240 minutes in both human and rat liver microparticles[1].
CHF6333 (10 μM, 4 h) xinafoate shows a 60.0% binding rate to human plasma proteins and a 58.0% binding rate to rat plasma proteins[1].
CHF6333 (1 μM, 1 h) xinafoate remains more than 80% unmetabolized after incubation for 1 hour in rat or human lung S9 fractions[1].
CHF6333 (0.014-10 μM) xinafoate exhibits IC50 values greater than 10 μM for all CYP450 isoenzymes (CYP1A1, CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4, and CYP3A5)[1].
CHF6333 xinafoate shows an IC50 of 24.7 μM against acetylcholinesterase[1].
CHF6333 xinafoate exhibits an IC50 >100 against the M2 receptor and an IC50 of 67.3 μM against the M3 receptor[1].
CHF6333 (100 μM) xinafoate does not inhibit hERG channels in HEK-293 cells and posed no risk of cardiovascular toxicity[1].
CHF6333 (1-100 μM, 24 h) xinafoate shows no cytotoxicity to SAEC (human airway epithelial cells) and HepG2 (human liver cancer cells) at high concentrations, demonstrating good safety[1].
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.
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Animal Model:Sprague-Dawley (SD) rats were induced to have acute lung injury and pulmonary hemorrhage by direct intratracheal (intratracheal) injection of exogenous human neutrophil elastase (NE, 100 U/rat)[1].
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Dosage:0.03 mg/kg, 0.3 mg/kg, 0.6 mg/kg
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Administration:Intratracheal, once
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Result:Significantly reduced hemoglobin concentration in BALF (i.e., pulmonary hemorrhage) in a dose-dependent manner.
Chemical Information
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No. CAS 3071964-44-5
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Peso molecular 728.72
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Fòrmula C38H35F3N6O6
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SMILES
FC(F)(C1=CC=CC(N2C(C)=C([C@H](N3C2=NNC3=O)C4=C(C=C(C=C4)C#N)CC[N+](C)(C)C)C(OC)=O)=C1)F.OC5=C(C=CC6=C5C=CC=C6)C([O-])=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHF-6333 xinafoate Related Classifications
HY-179566A Related Classifications
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