CHF-6333 chloride
CHF-6333 chloride is a neutrophil elastase (NE) inhibitor (IC50 = 0.21 nM; KD = 0.16 nM). CHF-6333 chloride retains its activity in both human (IC50 = 0.22 nM) and rat (IC50 = 3.63 nM) proteases. CHF-6333 chloride exhibits inhibitory activity against Proteinase 3 (IC50 = 22 nM). CHF-6333 chloride can be used for the study of bronchiectasis (BE).
For research use only. We do not sell to patients.
- CAS No.: 1613621-55-8
- Formula: C27H28ClF3N6O3
- Molecular Weight:577.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
CHF-6333 (Compound 15) (1 μM, 0-30 min) chloride exhibits a half-life (t1/2) greater than 240 minutes in both human and rat liver microparticles[1].
CHF-6333 (10 μM, 4 h) chloride shows a 60.0% binding rate to human plasma proteins and a 58.0% binding rate to rat plasma proteins[1].
CHF-6333 (1 μM, 1 h) chloride remains more than 80% unmetabolized after incubation for 1 hour in rat or human lung S9 fractions[1].
CHF-6333 (0.014-10 μM) chloride exhibits IC50 values greater than 10 μM for all CYP450 isoenzymes (CYP1A1, CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4, and CYP3A5)[1].
CHF-6333 chloride shows an IC50 of 24.7 μM against acetylcholinesterase[1].
CHF-6333 chloride exhibits an IC50 >100 against the M2 receptor and an IC50 of 67.3 μM against the M3 receptor[1].
CHF-6333 (100 μM) chloride does not inhibit hERG channels in HEK-293 cells and posed no risk of cardiovascular toxicity[1].
CHF-6333 (1-100 μM, 24 h) chloride 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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CAS No. 1613621-55-8
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Molecular Weight 577.00
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Formula C27H28ClF3N6O3
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SMILES
COC(C([C@@H](C1=C(C=C(C=C1)C#N)CC[N+](C)(C)C)N23)=C(C)N(C4=CC(C(F)(F)F)=CC=C4)C2=NNC3=O)=O.[Cl-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHF-6333 chloride Related Classifications
HY-182465 Related Classifications
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