2. Metabolic Enzyme/Protease
  3. Elastase
  4. CHF-6333

CHF-6333 is a neutrophil elastase (NE) inhibitor (IC50 = 0.21 nM; KD = 0.16 nM). CHF-6333 retains its activity in both human (IC50 = 0.22 nM) and rat (IC50 = 3.63 nM) proteases. CHF-6333 exhibits inhibitory activity against Proteinase 3 (IC50 = 22 nM). CHF-6333 can be used for the study of bronchiectasis (BE).

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CHF-6333

CHF-6333 Chemical Structure

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CHF-6333 Related Antibodies

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Description

CHF-6333 is a neutrophil elastase (NE) inhibitor (IC50 = 0.21 nM; KD = 0.16 nM). CHF-6333 retains its activity in both human (IC50 = 0.22 nM) and rat (IC50 = 3.63 nM) proteases. CHF-6333 exhibits inhibitory activity against Proteinase 3 (IC50 = 22 nM). CHF-6333 can be used for the study of bronchiectasis (BE)[1].

In Vitro

CHF-6333 (Compound 15) (1 μM, 0-30 min) exhibits a half-life (t1/2) greater than 240 minutes in both human and rat liver microparticles[1].
CHF-6333 (10 μM, 4 h) 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) remains more than 80% unmetabolized after incubation for 1 hour in rat or human lung S9 fractions[1].
CHF-6333 (0.014-10 μM) exhibits IC50 values greater than 10 μM for all CYP450 isoenzymes (CYP1A1, CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4, and CYP3A5)[1].
CHF-6333 shows an IC50 of 24.7 μM against acetylcholinesterase[1].
CHF-6333 exhibits an IC50 >100 against the M2 receptor and an IC50 of 67.3 μM against the M3 receptor[1].
CHF-6333 (100 μM) does not inhibit hERG channels in HEK-293 cells and posed no risk of cardiovascular toxicity[1].
CHF-6333 (1-100 μM, 24 h) 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.

CHF-6333 Related Antibodies
In Vivo

CHF-6333 (0.03-0.6 mg/kg, intratracheal, once) 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.
Clinical Trial
Molecular Weight

764.75

Formula

C38H39F3N6O8
SMILES

CC(N1C2=CC(C(F)(F)F)=CC=C2)=C([C@H](N3C1=NNC3=O)C4=C(C=C(C=C4)C#N)CC[N+](C)(C)C)C(OC)=O.OC5=C(C=CC6=CC=CC=C65)C([O-])=O.O.O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CHF-6333 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CHF-6333CHF6333CHF 6333ElastaseNeutrophil Elastase InhibitorBronchiectasisInhibitorinhibitorinhibit

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