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.
For research use only. We do not sell to patients.
- Formula: C30H31N3O3
- Molecular Weight:481.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
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.
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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Molecular Weight 481.59
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Formula 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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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)