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Cat. No.: HY-183286

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DHFR-IN-27

DHFR-IN-27 (Compound LA4) is an orally active DHFR inhibitor and antimalarial agent, with a K_i 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.

Formula: C₂₀H₂₅ClN₄O₄
Molecular Weight:420.89

Storage:

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

DHFR-IN-27 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Toxoplasma

0.44 nM (IC₅₀)

TgDHFR

1.71 nM (Ki)

All Parasite Isoforms :

In Vitro

DHFR-IN-27 potently inhibits purified TgDHFR-TS with a K_i 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.

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).

Chemical Information

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

Handling Instructions (2659 KB)

References

[1]. Decharuangsilp S, et al. Repurpose antimalarials to target Toxoplasma gondii dihydrofolate reductase thymidylate synthase. Eur J Med Chem. 2026;313:118863. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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