CYP51-IN-22
CYP51-IN-22, the non-deuterated analog of CYP51-IN-23-d3 (HY-174353S), is a potent and broad-spectrum CYP51 inhibitor.CYP51-IN-22 inhibits Aspergillus fumigatum with a MIC80 of 1 μg/mL. CYP51-IN-22 can prevent fungal phase transformation and biofilm formation. CYP51-IN-22 exhibits anti-drug resistance activity and fungal activity, and shows excellent safety for cells and significant pharmacological activity in mice. CYP51-IN-22 can be used for the study of invasive fungal infections (IFIs).
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: C29H30BrF2N7O2
- 分子量:626.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
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CYP51 |
体外実験
CYP51-IN-22 (Compound V23) (1-16 mL, 48 h) shows broad-spectrum activity against eight fluconazole-resistant fungi with a MIC80 of 1-16 μg/ml[1].
CYP51-IN-22 (2-8×MIC, 0-24 h) exhibits fungicidal activity in a dose-dependent manner against C. parapsilosis: The longer the time, the higher the concentration, and the better the fungicidal activity[1].
CYP51-IN-22 (0-32 mL, 6 h) shows effectiveanti-biofilm inhibition activity in the biofilm growth stage of C. glabrata and C. neoformans[1].
CYP51-IN-22 (2-8 mL, 4 h) can inhibit the phase transition of C. albicans[1].
CYP51-IN-22 (10 μM, 4 h) has no significant toxicity effect on HUVEC (human umbilical vein endothelial cell line) and SH-SY5Y (neuroblastoma cell line) [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:Candida parapsilosis was injected through the tail vein to establish a mouse (ICR, 4-6 weeks) candida-infection model
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Dosage:5 mg/kg, 10 mg/kg
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Administration:Intraperitoneal injection (i.p.) or gavage (p.o.) 4 h after infection
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Result:Reduced the renal fungal load in mice and was better than the positive control fluconazole.
Dose-dependent, and the efficacy of intraperitoneal injection was better than that of oral gavage administration.
化学情報
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分子量 626.50
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分子式 C29H30BrF2N7O2
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SMILES
FC1=CC(F)=CC=C1C(CN(C)CC2=CC=C(N3CCN(C(C4=CC(Br)=CC=C4)=O)CC3)C=C2)(O)CN5C=NN=N5
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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)