1. Anti-infection
  2. Fungal
  3. E1210

E1210 (Synonyms: APX001A)

Cat. No.: HY-18233 Purity: 99.30%
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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 182 In-stock
Estimated Time of Arrival: December 31
5 mg USD 165 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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

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].

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

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (279.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.30%

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Keywords:

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

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E1210
Cat. No.:
HY-18233
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