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

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.

For research use only. We do not sell to patients.

DHFR-IN-27

DHFR-IN-27 Chemical Structure

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DHFR-IN-27 Related Antibodies

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Description

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)

In Vitro

DHFR-IN-27 potently inhibits purified TgDHFR-TS with a Ki value of 1.71 nM[1].
DHFR-IN-27 (4 days) potently inhibits Toxoplasma gondii RH-GFP tachyzoites in HFF cells, with an IC50 of 0.44 nM, and exhibits a cell selectivity index as high as 165,000 relative to HFF cells[1].

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

DHFR-IN-27 Related Antibodies
In Vivo

LA4 (30 mg/kg; p.o.; daily; 4 days) demonstrates potent in vivo anti-toxoplasmosis activity, reducing T. gondii burden in peritoneal fluid and blood and extending infected mice median survival to day 15[1].

MedChemExpress (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).
Molecular Weight

420.89

Formula

C20H25ClN4O4
SMILES

O=C(OCC/1)C1=C\C(C=C2)=CC=C2OCCCOC3=C(N)N=C(N)N=C3CC.Cl
Shipping

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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DHFR-IN-27 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:

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

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