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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C38H39F3N6O8
- 分子量:764.75
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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 |
化学情報
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分子量 764.75
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CHF-6333 関連分類
HY-179566 関連分類
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