Antiparasitic agent-28
Antiparasitic agent-28 is an orally active, selective inhibitor of Toxoplasma gondii phenylalanine tRNA synthetase (TgcPheRS) with blood-brain barrier penetration. Antiparasitic agent-28 inhibits the growth of T. gondii tachyzoites (TgME49-Fluc strain) an (EC50 = 1 nM) and T. gondii bradyzoites (Tg68nLuc strain) induced by alkaline (EC50 = 3 nM) and glutamine-rich medium (EC50 = 0.1 nM). Antiparasitic agent-28 demonstrates potent anti-toxoplasmosis efficacy in mice infected with TgME49-Fluc tachyzoites. Antiparasitic agent-28 can be used for the study of Toxoplasma gondii infection.
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- Fòrmula: C30H31N3O3
- Peso molecular:481.59
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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
Antiparasitic agent-28 (Compound 12) (72 h) potently inhibits the growth of Toxoplasma gondii tachyzoites (TgME49-Fluc strain) (EC50 = 1 nM, EC90 = 2 nM)[1].
Antiparasitic agent-28 (96 h) effectively inhibits the growth of T. gondii bradyzoites (Tg68nLuc strain) induced by alkaline (EC50 = 3 nM) and glutamine-rich medium (EC50 = 0.1 nM)[1].
Antiparasitic agent-28 exhibits low toxicity to human hepatic HepG2 cells (CC50 = 0.99 μM, SI = CC50/EC50 = 1447) and human monocytic THP-1 cells (CC50 = 0.25 μM, SI = 374)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
Antiparasitic agent-28 (3 mg/kg, p.o., twice daily, 14 days) significantly prolongs the survival time in interferon gamma receptor 1 knockout mice infected with TgME49-Fluc tachyzoites[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/BL6 female mice (6-8 weeks old) infected with 300 TgME49-Fluc tachyzoites via intraperitoneal injection[1]
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Dosage:3 mg/kg
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Administration:p.o., twice daily, 7 days
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Result:Prevented chronic infection (no parasite outgrowth in brain homogenate).
Did not cause significant changes in plasma levels of liver and kidney function indicators (ALT, AST, BUN, creatinine).
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Animal Model:Interferon gamma receptor 1 knockout (Ifngr1⁻/⁻) mice infected with 300 TgME49-Fluc tachyzoites via i.p. injection[1]
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Dosage:3 mg/kg
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Administration:p.o., twice daily, 14 days
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Result:Prolonged the survival time (longer than that of the sulfadiazine-treated group).
Chemical Information
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Peso molecular 481.59
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Fòrmula C30H31N3O3
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SMILES
O=C(N1C[C@]([C@@H](C2=CC=C(C#CC3=CC=CC=C3O)C=C2)CC4)([H])N4CCC1)NC5=CC=C(OC)C=C5
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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.
Protocolo
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antiparasitic agent-28 Related Classifications
HY-175648 Related Classifications
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