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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- Formule: C38H39F3N6O8
- Masse moléculaire:764.75
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Masse moléculaire 764.75
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Formule C38H39F3N6O8
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHF-6333 Related Classifications
HY-179566 Related Classifications
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