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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 2422053-29-8
- 화학식: C23H24N4O4
- 분자량:420.46
-
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
- Protocol
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
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 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 | Cmax | Tmax | AUClast | T1/2 |
|---|---|---|---|---|---|---|---|
| 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
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 No. 2422053-29-8
-
분자량 420.46
-
화학식 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
-
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)
Debio 1453 Related Classifications
HY-178347 Related Classifications
Powered by Bioz