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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C20H25ClN4O4
- 分子量:420.89
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
[1]|
Toxoplasma 0.44 nM (IC50) |
TgDHFR 1.71 nM (Ki) |
体外実験
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.
体内実験
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).
化学情報
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分子量 420.89
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)