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Art. -Nr.: HY-178347

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Debio 1453

Debio 1453 is a bactericidal FabI inhibitor potent against N. gonorrhoeae (IC₅₀ = 0.6 nM), including drug-resistant strains. Debio 1453 demonstrates a low propensity for resistance selection and is effective in eradicating both planktonic and intracellular bacteria through a mechanism of concurrently inhibiting FabI and engaging the non-mutable NADH cofactor. Debio 1453 clears antibiotic-resistant N. gonorrhoeae infection in a murine vaginal model. Debio 1453 can be used for gonorrhoea research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2422053-29-8
Formel: C₂₃H₂₄N₄O₄
Molecular Weight:420.46

Speicherung:

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

Data Sheet (273 KB)

Debio 1453 Chemical Structure

CAS. Nr.: 2422053-29-8

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

Biologische Aktivität

Beschreibung

In Vitro

Debio 1453 shows activity against 2024 World Health Organisation N. gonorrhoeae reference strains that include strains resistant to Ceftriaxone (HY-B0712), Azithromycin (HY-17506), Spectinomycin (HY-B0438), Tetracycline (HY-A0107) and Ciprofloxacin (HY-B0356), with MIC range 0.03-0.125 μg/mL^[1].
Debio 1453 exhibits potent in vitro activity (MIC₅₀/MIC₉₀ = 0.06 μg/mL) against 100 contemporary clinical N. gonorrhoeae isolates, with MICs ranging from 0.008 to 0.125 μg/mL^[1].
Debio 1453 (0-16x MIC, 0-24 h) displays rapid bactericidal killing against both antibiotic-susceptible and extensively drug-resistant (XDR) N. gonorrhoeae in a time-dependent manner^[1].
Debio 1453 (0-8x MIC, 0-24 h) is effective against both internalised antibiotic-susceptible (ATCC 49226) and XDR N. gonorrhoeae (WHO X), eradicating the bacteria to the limit of detection within 24 h for each isolate tested (≥3.1 log10 CFU/mL and ≥2.8 log10 CFU/mL reductions, respectively)^[1].
Debio 1453 (4x-16x MIC) exhibits a low propensity for selecting mutants with reduced susceptibility in N. gonorrhoeae in vitro, thus validating FabI as its target^[1].
Debio 1453 (0.3-30 μM, 24 h) exhibits no cytotoxicity or negative impact on cell viability in HepG2 cells, and no clastogenic or aneugenic activity in lymphocytes irrespective of the presence or absence of a rat liver metabolic activation system^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

human hepatocytes (HepG2)
Concentration:

0.3, 1, 3, 10, and 30 μM
Incubation Time:

24 h
Result:

Showed no cytotoxicity or negative impact on cell viability at all concentrations tested, including the highest concentration of 30 μM.

Parmacokinetics

Species	Dose	Route	Note	C_max	T_max	AUC_last	T_1/2
Mice^[1]	80 mg/kg	p.o.	N.gonorrhoeae-infected mice	13800 ng/mL	1 h	54300 ng·h/mL	2.52 h

In Vivo

Debio 1453 (10-160 mg/kg (dosed as Debio 1453 P), p.o., twice daily for 2 days) shows potent efficacy in murine models of both N. gonorrhoeae vaginal infection and S. aureus thigh infection^[1].

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

Animal Model:

Ovariectomized BALB/c female mice (5-6 weeks) infected intravaginally with N. gonorrhoeae strains^[1]
Dosage:

10, 20, 30, 40, 80, and 160 mg/kg (dosed as Debio 1453 P)
Administration:

p.o., twice daily for 2 days
Result:

Demonstrated efficacy against all tested strains, producing clear dose-response relationships.
Achieved ~3 log10 CFU/mL reductions as compared to the start of treatment (0 h) and eradicated N. gonorrhoeae to the limit of detection by 48 h at multiple dose levels.

Animal Model:

Neutropenic female ICR mice infected intravaginally with S. aureus^[1]
Dosage:

10, 20, 30, 40, and 80 mg/kg (dosed as Debio 1453 P)
Administration:

p.o., twice daily for 2 days
Result:

Achieved >1 log10 CFU/mL reductions in thighs at 24 h and >2 log10 CFU reductions at 48 h, displaying efficacy comparable to a supratherapeutic dose of Linezolid (HY-10394).

Chemical Information

CAS. Nr. 2422053-29-8
Molecular Weight 420.46
Formel C₂₃H₂₄N₄O₄
SMILES

CC1=C(OC2=C1C=CC=C2)CN(C(/C=C/C3=CN=C4NC([C@H]([C@H](NC4=C3)C)O)=O)=O)C
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gerusz V, et al. The bactericidal FabI inhibitor Debio 1453 clears antibiotic-resistant Neisseria gonorrhoeae infection in vivo. Nat Commun. 2025 Sep 18;16(1):8309. [Content Brief]

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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