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Art. -Nr.: HY-187934

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DX-619

DX-619 is an antibacterial agent. DX-619 inhibits bacterial type II topoisomerases, DNA gyrase (GyrA), and topoisomerase IV (GrlA). DX-619 can be used in research related to bacterial infections, pneumonia, and other conditions.

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CAS. Nr.: 431058-65-0
Formel: C₂₁H₂₄FN₃O₄
Molecular Weight:401.43

Speicherung:

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

DX-619 Chemical Structure

CAS. Nr.: 431058-65-0

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

Bacterial InfectionFungal InfectionOthers

Bacterial Infection

Fungal Infection

DX-619 (20-48 h) exhibits the most potent antibacterial activity against Gram-positive bacteria among the tested compounds, including Ciprofloxacin (HY-B0356)-resistant MRSA (MIC₉₀ 0.5 μg/mL), MRCNS, VRE, and Ciprofloxacin (HY-B0356)-resistant S. pneumoniae^[2].

Bacterial Infection

DX-619 (20 h) exhibits good antibacterial activity against Gram-negative bacteria, including Haemophilus influenzae, Moraxella catarrhalis, Enterobacteriaceae, and Acinetobacter species^[2].
DX-619 (24 h) exhibits potent in vitro activity against Staphylococcus aureus and coagulase-negative staphylococci, with MIC₅₀ values of 0.06 and 0.016 μg/mL, respectively^[3].
DX-619 (24 h) inhibits Vancomycin (HY-B0671)-resistant Staphylococcus aureus strains (Hershey VRS2 and Michigan VRS1) with MIC values of 0.25 and 0.12 μg/mL, respectively^[3].
DX-619 (24 h) exhibits bactericidal activity against all 13 of 13 staphylococcal strains (including VRSA) after 24 h at 4× MIC, and shows bactericidal activity against VRSA strains after 3 to 6 h at 2× MIC^[3].
DX-619 exhibits activity against Imipenem (HY-B1369A)-resistant Bacteroides fragilis group strains, inhibiting 90.9% at ≤1 μg/mL, with an MIC₉₀ of 1 μg/mL^[5].
DX-619 exhibits activity against levofloxacin (HY-B0330)-resistant anaerobic Gram-positive cocci, with an MIC₉₀ of 2 μg/mL and 100% susceptibility at ≤2 μg/mL^[5].
DX-619 exhibits high activity against Clostridium species associated with gas gangrene, inhibiting all strains at MICs of ≤0.03 to 0.25 μg/mL^[5].
DX-619 exhibits activity against Moxifloxacin (HY-66011A)-resistant Clostridium difficile strains, with MICs ranging from 0.5 to 2 μg/mL^[5].

Others

DX-619 (12.5-200 μM; 5-30 min) is a mechanism-based inhibitor of CYP3A4 in human liver microsomes, with a K_I of 67.9 μM and a k_inact of 0.0730 min^-1^[1].
DX-619 inhibits OAT3-mediated 6β-OHF uptake with a K_i of 239 μM^[1].
DX-619 inhibits MATE1-mediated 6β-OHF uptake with a K_i of 4.32 μM^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2
Mice^[6]	10 mg/kg mg/kg	i.p.	1.26 μg/mL	0.25 h	0.56 h
Mice^[6]	10 mg/kg mg/kg	i.p.	5.99 μg/mL	0.25 h	0.63 h

In Vivo

Bacterial Infection

DX-619 (10 mg/kg; i.p.; twice daily; 14 days) is effective against penicillin-sensitive S. pneumoniae in a mouse pneumonia model, with an ED₅₀ of 9.15 mg/kg/day, and reduces lung viable bacterial counts to 1.75 log₁₀ CFU/mL^[6].
DX-619 (10 mg/kg; i.p.; twice daily; 14 days) is highly effective against penicillin-resistant S. pneumoniae in a mouse pneumonia model, with an ED₅₀ of 0.69 mg/kg/day, and reduces lung viable bacterial counts to 1.73 log₁₀ CFU/mL^[6].

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

Animal Model:

CBA/J (female, 5-week-old, 16-20 g, intranasal inoculation of PSSP strain NU83127)^[6]
Dosage:

Various doses (ED₅₀ determination); 10 mg/kg (bacteriological study)
Administration:

i.p.; twice daily (ED₅₀ determination); at 24, 36, and 48 h after inoculation (bacteriological study); 14 days
Result:

Achieved an ED₅₀ of 9.15 mg/kg/day against PSSP pneumonia.
Reduced mean viable bacterial counts in lungs to 1.75 log10 CFU/mL.
Eradicated viable bacteria from four of seven murine lungs.

Animal Model:

CBA/J (female, 5-week-old, 16-20 g, intranasal inoculation of PRSP strain NU187)^[6]
Dosage:

Various doses (ED₅₀ determination); 10 mg/kg (bacteriological study)
Administration:

i.p.; twice daily (ED₅₀ determination); at 24, 36, and 48 h after inoculation (bacteriological study); 14 days
Result:

Achieved an ED₅₀ of 0.69 mg/kg/day against PRSP pneumonia.
Reduced mean viable bacterial counts in lungs to 1.73 log10 CFU/mL.
Eradicated viable bacteria from four of seven murine lungs.

Related Protocols :

Research Protocol for Infectious Diseases

Chemical Information

CAS. Nr. 431058-65-0
Molecular Weight 401.43
Formel C₂₁H₂₄FN₃O₄
SMILES

COC1=C2N([C@H]3[C@H](C3)F)C=C(C(C2=CC=C1N4C[C@H](C5(CC5)N)CC4)=O)C(O)=O
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]. Imamura Y, et al. Effect of the fluoroquinolone antibacterial agent DX-619 on the apparent formation and renal clearances of 6β-hydroxycortisol, an endogenous probe for CYP3A4 inhibition, in healthy subjects. Pharmaceutical research. 2013 Feb;30(2):447-57.

[2]. Fujikawa K, et al. In vitro antibacterial activity of DX-619, a novel des-fluoro(6) quinolone. Antimicrobial agents and chemotherapy. 2005 Jul;49(7):3040-5. [Content Brief]

[3]. Bogdanovich T, et al. Antistaphylococcal activity of DX-619, a new des-F(6)-quinolone, compared to those of other agents. Antimicrobial agents and chemotherapy. 2005 Aug;49(8):3325-33. [Content Brief]

[4]. Sarapa N, et al. Lack of effect of DX-619, a novel des-fluoro(6)-quinolone, on glomerular filtration rate measured by serum clearance of cold iohexol. Antimicrobial agents and chemotherapy. 2007 Jun;51(6):1912-7.

[5]. Tanaka K, et al. In vitro antianaerobic activity of DX-619, a new des-fluoro(6) quinolone. Antimicrobial agents and chemotherapy. 2006 Nov;50(11):3908-13.

[6]. Fukuda Y, et al. In vivo efficacies and pharmacokinetics of DX-619, a novel des-fluoro(6) quinolone, against Streptococcus pneumoniae in a mouse lung infection model. Antimicrobial agents and chemotherapy. 2006 Jan;50(1):121-5.

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.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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DX-619

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