KGDI-109
KGDI-109 is an orally active and selective Porphyromonas gingivalis dipeptidyl peptidase 7 (PgDPP7) inhibitor with an IC50 of 53.8 µM and a Ki of 25.1 µM. KGDI-109 is also a selective antibacterial agent that suppresses Porphyromonas gingivalis growth, reduces oral Porphyromonas gingivalis levels, and suppresses alveolar bone resorption. KGDI-109 preserves gut microbial diversity. KGDI-109 can be used for the research of periodontitis.
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- No. CAS: 3027146-73-9
- Fòrmula: C22H27N3O6
- Peso molecular:429.47
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
KGDI-109 (12.5-50 μM; 30 min) selectively inhibits DPP7 and DPP5 enzyme activity in Porphyromonas gingivalis W83 cells, with no effect on DPP4 or DPP11 activity[1].
KGDI-109 (0-200 μM; 24-72 h) selectively inhibits the growth of Porphyromonas gingivalis W83 with an MIC of 1.56 μM and MBC of 6.25 μM, and does not inhibit the growth of other tested oral bacteria at concentrations up to 200 μM[1].
KGDI-109 (200 μM; 0-24 h) significantly reduces Porphyromonas gingivalis W83 ATP activity[1].
KGDI-109 (25-200 μM; 48 h) significantly inhibits biofilm formation by Porphyromonas gingivalis[1].
KGDI-109 (100-200 μM; 24 h) does not reduce the viability of human oral epithelial Ca9-22 cells or human THP-1 macrophage-like cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human oral epithelial Ca9-22 cells, human monocyte-derived THP-1 macrophage-like cells
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Concentration:100; 200 μM
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Incubation Time:24 h
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Result:Had no significant effect on the viability of either Ca9-22 or THP-1 cells relative to untreated controls.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N/Crl mice (9-week-old male, 20-25 g) induced by P. gingivalis[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Showed no abnormalities in health status or body weight changes.
Significantly suppressed alveolar bone resorption.
Significantly reduced attachment loss in gingival tissue sections.
Decreased the number of TRAP-positive osteoclasts adjacent to the alveolar bone surface.
Significantly reduced the relative amount of P. gingivalis in the oral cavity while leaving total oral bacterial levels unchanged.
Maintained higher intestinal microbiota alpha diversity.
Chemical Information
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No. CAS 3027146-73-9
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Peso molecular 429.47
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Fòrmula C22H27N3O6
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SMILES
COC1=CC=C(C=C1)C[C@@H](C(OC(C)C)=O)NC([C@H](CC2=CC=C(C=C2)[N+]([O-])=O)N)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KGDI-109 Related Classifications
HY-184139 Related Classifications
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