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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1613621-55-8
- 화학식: C27H28ClF3N6O3
- 분자량:577.00
-
보관:
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]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
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
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 No. 1613621-55-8
-
분자량 577.00
-
화학식 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-]
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHF-6333 chloride Related Classifications
HY-182465 Related Classifications
Powered by Bioz