1. Metabolic Enzyme/Protease Anti-infection
  2. Dipeptidyl Peptidase Bacterial
  3. 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.

For research use only. We do not sell to patients.

KGDI-109

KGDI-109 Chemical Structure

CAS No. : 3027146-73-9

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Description

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[1].

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.

Cell Viability Assay[1]

Cell Line: Human oral epithelial Ca9-22 cells, human monocyte-derived THP-1 macrophage-like cells
Concentration: 100; 200 μM
Incubation Time: 24 h
Result: Had no significant effect on the viability of either Ca9-22 or THP-1 cells relative to untreated controls.
In Vivo

KGDI-109 (20 mg/kg; p.o.; daily; 7 days) significantly suppresses periodontal tissue destruction in a murine periodontitis model by reducing oral P. gingivalis levels, while maintaining intestinal microbial diversity[1].

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

Animal Model: C57BL/6N/Crl mice (9-week-old male, 20-25 g) induced by P. gingivalis[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 7 days
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.
Molecular Weight

429.47

Formula

C22H27N3O6

CAS No.
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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Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
KGDI-109
Cat. No.:
HY-184139
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