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  3. E1210

E1210 (Synonyms: APX001A)

Cat. No.: HY-18233
Handling Instructions

E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.

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

E1210 Chemical Structure

E1210 Chemical Structure

CAS No. : 936339-60-5

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Description

E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis[1][2].

IC50 & Target

Fungal[1][2]

In Vitro

E1210 inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50s of 0.3 to 0.6 μM but has no inhibitory activity against human Pig-Wp even at concentrations as high as 100 μM. To confirm the inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis, expression of ALS1 protein, a GPI-anchored protein, on the surfaces of C. albicans cells treated with E1210 is studied and shown to be significantly lower than that on untreated cells. E1210 inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC[1].

In Vivo

E1210 (2.5 mg/kg, 5 mg/kg and 10 mg/kg; oral administration; twice daily; for 3 days; specific-pathogen-free female ICR mice) treatment reduces the number of viable C. albicans cells in the oral cavity in a dose-dependent manner[2].

Animal Model: Specific-pathogen-free female ICR mice (5 weeks; ~25 g) with C. albicans[2]
Dosage: 2.5 mg/kg, 5 mg/kg and 10 mg/kg
Administration: Oral administration; twice daily; for 3 days
Result: Reduced the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.
Molecular Weight

358.39

Formula

C₂₁H₁₈N₄O₂

CAS No.

936339-60-5

SMILES

NC1=NC=CC=C1C2=CC(CC3=CC=C(COC4=NC=CC=C4)C=C3)=NO2

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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.

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Keywords:

E1210APX001AE 1210E-1210FungalGlycosylphosphatidylinositolfirst-in-classbroad-spectrumGwt1pdisseminatedInhibitorinhibitorinhibit

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E1210
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HY-18233
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