2. Anti-infection
  3. Parasite
  4. 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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Antiparasitic agent-28

Antiparasitic agent-28 Chemical Structure

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Antiparasitic agent-28 Related Antibodies

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Description

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[1].

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.

Antiparasitic agent-28 Related Antibodies
In Vivo

Antiparasitic agent-28 (Compound 12) (3 mg/kg, p.o., twice daily, 7 days) prevents chronic infection and in immunocompetent C57/BL6 female mice infected with TgME49-Fluc tachyzoites[1].
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.

Animal Model: C57/BL6 female mice (6-8 weeks old) infected with 300 TgME49-Fluc tachyzoites via intraperitoneal injection[1]
Dosage: 3 mg/kg
Administration: p.o., twice daily, 7 days
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).
Animal Model: Interferon gamma receptor 1 knockout (Ifngr1⁻/⁻) mice infected with 300 TgME49-Fluc tachyzoites via i.p. injection[1]
Dosage: 3 mg/kg
Administration: p.o., twice daily, 14 days
Result: Prolonged the survival time (longer than that of the sulfadiazine-treated group).
Molecular Weight

481.59

Formula

C30H31N3O3
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Antiparasitic agent-28 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Antiparasitic agent-28Antiparasitic agent28Antiparasitic agent 28ParasiteToxoplasma gondiiinfectionTgcPheRSTgME49-Fluc strainTg68nLuc strainInhibitorinhibitorinhibit

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