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Art. -Nr.: HY-182465

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CHF-6333 chloride

CHF-6333 chloride is a neutrophil elastase (NE) inhibitor (IC₅₀ = 0.21 nM; K_D = 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).

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CAS. Nr.: 1613621-55-8
Formel: C₂₇H₂₈ClF₃N₆O₃
Molecular Weight:577.00

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

CHF-6333 chloride Chemical Structure

CAS. Nr.: 1613621-55-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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.

In Vivo

CHF-6333 (0.03-0.6 mg/kg, intratracheal, once) chloride can effectively prevent lung tissue damage directly caused by NE in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage:

0.03 mg/kg, 0.3 mg/kg, 0.6 mg/kg
Administration:

Intratracheal, once
Result:

Significantly reduced hemoglobin concentration in BALF (i.e., pulmonary hemorrhage) in a dose-dependent manner.

Chemical Information

CAS. Nr. 1613621-55-8
Molecular Weight 577.00
Formel C₂₇H₂₈ClF₃N₆O₃
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-]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Armani E, et al. Design, Synthesis, and Biological Evaluation of the Novel Neutrophil Elastase Inhibitor CHF-6333 for the Inhaled Treatment of Bronchiectasis. J Med Chem. 2025 Dec 11;68(23):24869-24889. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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