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

Antiparasitic agent-28 是一种口服活性的、选择性抑制 Toxoplasma gondii 苯丙氨酸 tRNA 合成酶 (TgcPheRS) 的抑制剂,具有血脑屏障渗透能力。Antiparasitic agent-28 抑制 T. gondii 速殖子 (TgME49-Fluc 株) 的生长 (EC50 = 1 nM) 以及碱性诱导的 T. gondii 缓殖子 (Tg68nLuc 株) (EC50 = 3 nM) 和富含谷氨酰胺培养基诱导的缓殖子 (EC50 = 0.1 nM)。Antiparasitic agent-28 在感染 TgME49-Fluc 速殖子的小鼠中显示出强大的抗弓形虫病疗效。Antiparasitic agent-28 可用于研究 Toxoplasma gondii 感染。

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Antiparasitic agent-28

Antiparasitic agent-28 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Antiparasitic agent-28 (Compound 12) (72 h) 强效抑制 Toxoplasma gondii 速殖子 (TgME49-Fluc 株) 的生长 (EC50 = 1 nM, EC90 = 2 nM)[1]
Antiparasitic agent-28 (96 h) 有效抑制碱性诱导的 T. gondii 缓殖子 (Tg68nLuc 株) (EC50 = 3 nM) 和富含谷氨酰胺培养基诱导的缓殖子 (EC50 = 0.1 nM)[1]
Antiparasitic agent-28 对人肝细胞 HepG2 细胞 (CC50 = 0.99 μM, SI = CC50/EC50 = 1447) 和人单核细胞 THP-1 细胞 (CC50 = 0.25 μM, SI = 374) 表现出低毒性[1]

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

体内研究
(In Vivo)

Antiparasitic agent-28 (Compound 12) (3 mg/kg,口服,每日两次,7 天) 可阻止感染 TgME49-Fluc 速殖子的 C57/BL6 雌性小鼠引起的慢性感染[1]
Antiparasitic agent-28 (3 mg/kg,口服,每日两次,14 天) 显著延长感染 TgME49-Fluc 速殖子的干扰素 γ 受体 1 敲除小鼠的存活时间[1]

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).
分子量

481.59

Formula

C30H31N3O3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

Antiparasitic agent-28 相关分类

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  • 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.

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Antiparasitic agent-28
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HY-175648
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