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

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.

For research use only. We do not sell to patients.

CYP51-IN-25 Chemical Structure

CYP51-IN-25 Chemical Structure

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Description

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].

In Vitro

CYP51-IN-25 (Compoud C52) has a broad-spectrum antifungal activity in Candida albicans (SC 5314) (MIC80 = 0.0625 μg/mL), Candida albicans (CPCC 400616) (MIC80 = 0.0625 μg/mL), Candida tropicalis (CGMCC 2.3739) (MIC80 = 0.0625 μg/mL), Candida parapsilosis (GIM 2.190) (MIC80 = 0.0625 μg/mL), Candida glabrata (Clinical isolation) (MIC80 = 0.0125 μg/mL) (MFC = 0.5 μg/mL), Candida krusei (AS 2.1045) (MIC80 = 0.0125 μg/mL) (MFC = 0.0125 μg/mL), Cryptococcus neoformans (CGMCC 2.3161) (MIC80 = 0.0125 μg/mL) (MFC = 0.0625 μg/mL) and Aspergillus fumigatus (CGMCC 3.7795) (MIC80 = 0.025 μg/mL)[1].
CYP51-IN-25 has a lower risk of drug-drug interactions (DDI) in other CYP450 isoforms such as 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 maintains a favorable safety profile toward mammalian cells within the tested concentration range[1].
CYP51-IN-25 inhibits the biofilm formation of Candida glabrata (SMIC50 = 0.0625 μg/mL) and Cryptococcus neoformans (CGMCC 2.3161) (SMIC50 = 0.1625 μg/mL)[1].
CYP51-IN-25 (2 μg/mL) effectively inhibits the transformation of fungi from yeast phase to hyphal phase[1].
CYP51-IN-25 (16 μg/mL,48 h) destroys the integrity of fungal cell membranes of Candida albicans (SC 5314)[1].
CYP51-IN-25 (0.0125-0.125 μg/mL) can significantly reduce the content of ergosterol of Candida albicans (SC 5314) and Cryptococcus neoformans (CGMCC 2.3161)[1].

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

In Vivo

CYP51-IN-25 (500 mg/kg; i.g.) has favorable safety profile under acute exposure conditions in the ICR mice female and male mice[1].
CYP51-IN-25 (100 mg/kg; i.g.; once daily; for 14 days) exhibits low cumulative toxicity under subacute exposure conditions in the ICR mice female and male mice[1].
CYP51-IN-25 (1-10 mg/kg; i.g.; once daily; for 5 days) has strong antifungal activity and prolongs the survival cycle of mice in a Candida albicans (SC 5314) infectious mice[1].

MedChemExpress (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.
Molecular Weight

535.52

Formula

C27H22D3F5N4O2

SMILES

FC1=CC=C([C@]([C@H](C)N(C([2H])([2H])[2H])CC2=CC=C(C3=CC=C(OC(F)(F)F)C=C3)C=C2)(O)CN4C=NC=N4)C(F)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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Product Name:
CYP51-IN-25
Cat. No.:
HY-174394S
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