Pirtenidine free base
Pirtenidine free base is a broad-spectrum antibacterial and anti-plaque agent. Pirtenidine free base exhibits bactericidal activity against oral plaque bacteria in vitro and inhibits plaque formation. Pirtenidine free base inhibits the growth, budding, germ tube formation and buccal epithelial cell adhesion of Candida albicans and Saccharomyces cerevisiae, reduces the oxygen uptake rate of yeast, and impairs mitochondrial respiratory function. Pirtenidine free base disrupts the integrity of fungal cell wall and membrane, leading to cytoplasmic leakage, cell shrinkage, and lysis. Pirtenidine free base binds tightly to mucosal surfaces in vivo with low systemic exposure. Pirtenidine free base can be used in studies related to dental plaque, fungal infections and oral candidiasis.
For research use only. We do not sell to patients.
- CAS No.: 103923-27-9
- Formula: C21H38N2
- Molecular Weight:318.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Pirtenidine (compound 11) (30 min) free base potently kills Streptococcus mutans 6715-13 in an in vitro dental plaque model, with an MBC of 0.28 mM[1].
Pirtenidine (2 min daily) free base exhibits potent in vitro bactericidal activity against dental plaque, specifically Streptococcus mutans 6715-13 (CC = 9.1, PBI = 2.8) and Actinomyces viscosus M-100 (CC = 6.9, PBI = 2.8)[1].
Pirtenidine (2 minutes daily) free base exhibits bactericidal activity against a variety of oral plaque-forming microorganisms in an in vitro dental plaque model, with CC values ranging from 1.6 to 18.3 for the tested strains[1].
Pirtenidine (0.2-800 mg/l; 24 h) free base exhibits antifungal activity against C. albicans KCCC 14172, C. tropicalis KCCC 13622, C. pseudotropicalis KCCC 13709, C. albicans ATCC 10231, and S. cerevisiae NCYC 975, with MIC values ranging from 1.5 to 3.0 mg/l. It also displays fungicidal activity, with MCC values of 12.5-25 mg/l for Candida strains, while the MCC value of S. cerevisiae is consistent with its MIC value[2].
Pirtenidine (0.75-3.0 mg/l; sampling every 60 min) free base inhibits the growth of C. albicans KCCC 14172 and S. cerevisiae NCYC 975 in a concentration-dependent manner[2].
Pirtenidine (0.75-3.0 mg/l) free base inhibits the budding of C. albicans KCCC 14172 and S. cerevisiae NCYC 975; its activity is comparable to that of Octenidine (HY-B2170) when incubated in Eagle's medium[2].
Pirtenidine (0.75-3.0 mg/l) free base blocks germ tube formation of C. albicans KCCC 14172 during incubation in calf serum, and its activity is comparable to that of Octenidine[2].
Pirtenidine (0.75-3.0 mg/l; interval sampling) free base induces concentration-dependent leakage of cytoplasmic substances in C. albicans KCCC 14172 and S. cerevisiae NCYC 975, with a more significant leakage level observed in S. cerevisiae[2].
Pirtenidine (1.5 mg/l; 1-24 h) free base causes progressive cell envelope damage, lysis, and cytoplasmic coagulation in C. albicans KCCC 14172 and S. cerevisiae NCYC 975[2].
Pirtenidine (0.25-0.5 × MIC; 1-24 h) free base inhibits the adhesion of Candida albicans ATCC 10231, Candida albicans KCCC 14172, Candida tropicalis KCCC 13622, and Candida pseudotropicalis KCCC 13709 to human oral buccal epithelial cells in vitro[3].
Pirtenidine (0.5 × MIC; 30 min) free base reduces the adhesion of Candida albicans KCCC 14172 to human oral buccal epithelial cells in vitro[3].
Pirtenidine (0.25 × MIC-MIC; 60-180 min) free base inhibits germ tube formation of Candida albicans KCCC 14172 in vitro at both sub-inhibitory and inhibitory concentrations[3].
Pirtenidine (0.5 × MIC; 12-24 h, during adherence assay) free base inhibits the adhesion of stationary-phase and log-phase Candida albicans KCCC 14172 to human oral buccal epithelial cells in vitro when added during either the growth phase or the adherence assay phase[3].
Pirtenidine free base does not induce petite colony mutations in Saccharomyces cerevisiae cells, nor does it antagonize ethidium bromide-induced petite colony mutations[5].
Pirtenidine free base exhibits a MIC of 20 μg/mL against Saccharomyces cerevisiae N.C.Y.C. 239 cultured with glucose as the carbon source, while its MIC against the same strain cultured with sodium lactate as the carbon source is 4 μg/mL, indicating that its activity increases when mitochondrial function is required[5].
Pirtenidine (2 μg/mL) free base reduces the oxygen uptake rate of Saccharomyces cerevisiae N.C.Y.C. 239 cells in logarithmic growth phase by 47%[5].
Pirtenidine free base does not affect mitochondrial cytochrome synthesis in late-exponential-phase Saccharomyces cerevisiae N.C.Y.C. 239 cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC0-∞ | Vz | CL | T1/2 (Elimination) | T1/2 (Distribution) | Cmax | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[4] | 1.35 mg/kg | i.v. | 496 ng·h/mL | 8.62 L/kg | 2.72 L/h/kg | 2.2 h | 0.14 h | / | / | / |
| Rat[4] | 4.5 mg/kg | p.o. | / | / | / | / | / | / | / | 0.3 % |
| Dog[4] | 0.23 mg/kg | i.v. | 160 ng·h/mL | 3.31 L/kg | 1.50 L/h/kg | 1.53 h | 0.08 h | / | / | / |
| Dog[4] | 4.5 mg/kg | p.o. | 312 ng·h/mL | / | / | 2.1 h | / | 49.7 ng/mL | 5.0 h | 10 % |
Chemical Information
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CAS No. 103923-27-9
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Molecular Weight 318.55
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Formula C21H38N2
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SMILES
N(=C1C=CN(C=C1)CCCCCCCC)CCCCCCCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Pirtenidine
- 103923-27-9
- Bacterial
- Fungal
- Streptococcus sobrinus 6715-13
- Saccharomyces cerevisiae NCYC 975
- male Sprague-Dawley rats
- human buccal epithelial cells
- oral plaque-producing bacteria
- Actinomyces viscosus M-100
- Candida albicans KCCC 14172
- beagle dogs
- Candida tropicalis KCCC 13622
- Candida pseudotropicalis KCCC 13709
- Inhibitor
- inhibitor
- inhibit