2. Anti-infection Others
  3. Fungal Isotope-Labeled Compounds
  4. CYP51-IN-25

CYP51-IN-25是一种广谱抗真菌剂，MIC80 为 0.00625-0.05 μg/mL。CYP51-IN-25 是一种具有抗生素性质的氘化化合物。CYP51-IN25 可以抑制真菌 CYP51 酶，阻断麦角甾醇合成，破坏细胞膜完整性。CYP51-IN-25 可用于真菌感染的研究。

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CYP51-IN-25 Chemical Structure

CYP51-IN-25 Chemical Structure

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CYP51-IN-25 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CYP51-IN-25 is a orally active broad spectrum antifungal agent with the MIC80 of 0.00625-0.05 μg/mL. is a CYP51-IN-25 is a deuterated compound with antibiotic properties. CYP51-IN-25 can inhibit the fungal CYP51 enzyme, block ergosterol synthesis, and disrupt cell membrane integrity. CYP51-IN-25 can be used for research on fungal infections[1].

体外研究
(In Vitro)

CYP51-IN-25 (Compoud C52) (0.00625-3.2μg/mL) 具有广谱的抗菌活性，其中白色念珠菌 (SC 5314) (MIC80 = 0.0625 μg/mL)，白色念珠菌 (CPCC 400616) (MIC80 = 0.0625 μg/mL) (MFC = 0.0125 μg/mL)，热带念珠菌 (CGMCC 2.3739) (MIC80 = 0.0625 μg/mL)，近平滑念珠菌 (GIM 2.190) (MIC80 = 0.0625 μg/mL)，光滑念珠菌 (Clinical isolation) (MIC80 = 0.0125 μg/mL) (MFC = 0.5 μg/mL)，克柔念珠菌 (AS 2.1045) (MIC80 = 0.0125 μg/mL) (MFC = 0.0125 μg/mL)，新型隐球菌 (CGMCC 2.3161) (MIC80 = 0.0125 µg/mL) (MFC = 0.0625 μg/mL)和烟曲霉 (CGMCC 3.7795) (MIC80=0.025 μg/mL)[1]。
CYP51-IN-25 在其他 CYP450 亚型中具有较低的药物相互作用 (DDI) 风险，如 CYP1A2 (IC50 > 10 μg/mL)，CYP2C9 (IC50 = 1.76 μg/mL)，CYP2C19 (IC50 = 1.71 μg/mL)，CYP2D6 (IC50 > 10 μg/mL)，CYP3A4-M (IC50 = 5.11 μg/mL) and CYP3A4-T (IC50 = 6.62 μg/mL)[1]。
CYP51-IN-25 (72 h) 在测试浓度范围内对哺乳动物细胞保持良好的安全性[1]。
CYP51-IN-25 (24 h) 能抑制光滑念珠菌 (SMIC50=0.0625 μg/mL) 和新型隐球菌 (CGMCC 2.3161) (SMIC50 = 0.1625 μg/mL) 的生物膜形成[1]。
CYP51-IN-25 (2 μg/mL，4 小时) 能有效抑制真菌从酵母相向菌丝相的转化[1]。
CYP51-IN-25 (16 μg/mL，48 小时) 能破坏白色念珠菌 (SC 5314) 细胞膜的完整性[1]。
CYP51-IN-25 (0.0125-0.125 μg/mL，16 小时) 可显著降低白色念珠菌 (SC 5314) 和新型隐球菌 (CGMCC 2.3161) 的麦角甾醇含量[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CYP51-IN-25 相关抗体:
体内研究
(In Vivo)

CYP51-IN-25 (500 mg/kg；i.g.) 对于雌性和雄性 ICR 小鼠在急性暴露条件下具有良好的安全性[1]。
CYP51-IN-25 (100 mg/kg；i.g.；每日一次；持续 14 天) 对于雌性和雄性 ICR 小鼠在亚急性暴露条件下表现出低累积毒性[1]。
CYP51-IN-25 (1-10 mg/kg；i.g.；每日一次；持续 5 天) 具有很强的抗真菌活性，可延长白色念珠菌 (SC 5314) 感染小鼠的存活周期[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: the ICR mice female and male mice (6-8 weeks, 20-25g)[1]
Dosage: 500 mg/kg
Administration: Oral gavage (i.g.) 200 μL
Result: Did not cause significant changes in the weight and did not cause significant pathological changes in major organs of the infectious mice.
Animal Model: the ICR mice female and male mice (6-8 weeks, 20-25g)[1]
Dosage: 100 mg/kg
Administration: Oral gavage (i.g.); once daily; for 14 days
Result: Keeped the weight of mice fluctuating within a physiological range and did not cause significant histopathological changes in the liver and kidneys of the infectious mice.
Animal Model: 1×106 (CFU)/mL Candida albicans (SC5314) injected the male ICR mice (4-6 weeks, 18-22g)[1]
Dosage: 1 mg/kg, 5 mg/kg, 10 mg/kg, fluconazole (HY-B0101) as a control group
Administration: Oral gavage (i.g.); once daily for 5 days
Result: Exhibited strong antifungal activity and significantly reduced the amount of fungi in the kidneys.
分子量

535.52

Formula

C27H22D3F5N4O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CYP51-IN-25 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CYP51-IN-25FungalIsotope-Labeled CompoundsantifungalCYP51ergosterolinfectionInhibitorinhibitorinhibit

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