YL6113
YL6113 is a potent and selective dual inhibitor of metallo-β-lactamases (MBLs) and serine-β-lactamases (SBLs). YL6113 shows inhibitory effect to MBLs, such as NDm-1, VIM-2, IMP-1, with IC50 values of 0.25, 27.16 and 3.55 μM. YL6113 shows inhibitory effect to SBLs, such as KPC-2, AmpC, OXA-48, with IC50 values of 0.2, 34.1 and 1.31 μM. YL6113 enhances the antibacterial efficacy of Meropenem (HY-13678) against carbapenem-resistant Gram-negative bacteria. YL6113 can be used for the research of infection.
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- 화학식: C18H18BClN4O5
- 분자량:416.62
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Beta-lactamase Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
KPC-2 0.2 μM (IC50) |
NDM-1 0.25 μM (IC50) |
OXA-48 1.31 μM (IC50) |
IMP-1 3.55 μM (IC50) |
VIM-2 27.16 μM (IC50) |
AmpC 34.1 μM (IC50) |
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | Tmax | AUC0-t | MRT0-t | Vz | ClF_obs |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 0.88 h | 4779.52 μg/L | 0.08 h | 3670.17 μg/L·h | 1.01 h | 3.46 L/kg | 2.72 L/h/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine sepsis model infected with NDM-1-producing K.p. 140509 strain[1]
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Dosage:10 mg/kg
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Administration:Ip, a single dose
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Result:Significantly reduced bacterial load in the lungs, liver, and kidneys compared to the control and Meropenem-only groups.
Chemical Information
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분자량 416.62
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화학식 C18H18BClN4O5
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SMILES
NCC1=CC=C(C=C1)C2=CN(N=N2)CC3=CC=C4OCB(OC4=C3C(O)=O)O.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)