2. Metabolic Enzyme/Protease Anti-infection
  3. Dihydrofolate reductase (DHFR) Parasite
  4. DHFR-IN-27

DHFR-IN-27 (Compound LA4) 是一种具有口服活性的 DHFR 抑制剂和抗疟剂，对 TgDHFR 的 Ki 值为 1.71 nM。DHFR-IN-27 能够降低感染小鼠体内 Toxoplasma gondii 的寄生负荷，延长感染小鼠的存活时间。DHFR-IN-27 对 Toxoplasma gondii 发挥抗寄生虫 (Antiparasitic) 作用。DHFR-IN-27 可用于弓形虫病的研究。

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DHFR-IN-27

DHFR-IN-27 Chemical Structure

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DHFR-IN-27 相关抗体

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DHFR-IN-27 (Compound LA4) is an orally active DHFR inhibitor and antimalarial agent, with a Ki value of 1.71 nM against TgDHFR. DHFR-IN-27 reduces the parasitic load of Toxoplasma gondii in infected mice and prolongs the survival time of infected mice. DHFR-IN-27 exerts Antiparasitic effects against Toxoplasma gondii. DHFR-IN-27 can be used in the research of toxoplasmosis[1].

IC50 & Target[1]

Toxoplasma

0.44 nM (IC50)

TgDHFR

1.71 nM (Ki)

体外研究
(In Vitro)

DHFR-IN-27 可强效抑制纯化的 TgDHFR-TS，其 Ki 值为 1.71 nM[1]。
DHFR-IN-27 (4 天) 可强效抑制 HFF 细胞内的刚地弓形虫 RH-GFP 速殖子，其 IC50 为 0.44 nM，且相对于 HFF 细胞具有高达 165,000 的细胞选择性指数[1]。

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

DHFR-IN-27 相关抗体:
体内研究
(In Vivo)

LA4 (30 mg/kg；口服；每日一次；连续 4 天) 表现出强大的体内抗弓形虫活性，可降低 T. gondii 在腹腔液和血液中的载量，并将感染小鼠的中位生存期延长至第 15 天[1]。

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

Animal Model: ICR (female, 6-8 weeks old, infected intraperitoneally with 3000 Toxoplasma gondii RH (type I) tachyzoites)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 4 days
Result: Reduced mean parasitic burden in peritoneal fluid to <103 T. gondii copy number.
Significantly reduced mean parasitic burden in blood compared to vehicle control.
Extended median survival time to day 15, with first death event on day 11; survival differed significantly from vehicle control (adjusted p < 0.001), with a hazard ratio of 0.02 (95% CI 0.01, 0.05).
分子量

420.89

Formula

C20H25ClN4O4
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

DHFR-IN-27 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

DHFR-IN-27Dihydrofolate reductase (DHFR)Parasitehuman dihydrofolate reductaseToxoplasma gondiiT. gondii RH-GFP tachyzoitesHFF cellsTgDHFR-TSdihydrofolate reductasetoxoplasmosisEcΔFΔTΔtolC-TgDHFR-TS E. coliInhibitorinhibitorinhibit

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