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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C20H25ClN4O4
- Masse moléculaire:420.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Toxoplasma 0.44 nM (IC50) |
TgDHFR 1.71 nM (Ki) |
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.
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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Masse moléculaire 420.89
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DHFR-IN-27 Related Classifications
HY-183286 Related Classifications
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