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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C20H25ClN4O4
- Molecular Weight:420.89
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (female, 6-8 weeks old, infected intraperitoneally with 3000 Toxoplasma gondii RH (type I) tachyzoites)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 4 days
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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
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Molecular Weight 420.89
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Formel C20H25ClN4O4
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SMILES
O=C(OCC/1)C1=C\C(C=C2)=CC=C2OCCCOC3=C(N)N=C(N)N=C3CC.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)