| Field | Specification |
|---|---|
| Alternative names | APX001; E1211 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H21N4O6P |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Fosmanogepix, also known as APX001 and E1211, is a broad-spectrum agent against invasive fungal infections that targets the conserved Gwt1 enzyme required for localizing glycosylphosphatidylinositol-anchored mannoproteins in fungi. This inhibition prevents proper localization of cell wall mannoproteins, compromising cell wall integrity, biofilm formation, germ tube formation and fungal growth, and can be used in invasive fungal infection research[1]. It is supplied as a white to yellow solid (C22H21N4O6P, MW 468.40) at 99.26% purity.
Physical & Chemical Properties
| CAS Number | 2091769-17-2 |
|---|---|
| Molecular Formula | C22H21N4O6P |
| Molecular Weight | 468.40 g/mol |
| Purity | 99.26% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=P(OC[N+]1=CC=CC(C2=CC(CC3=CC=C(COC4=NC=CC=C4)C=C3)=NO2)=C1N)(O)[O-] |
| Signaling Pathway | Anti-infection |
| Solubility | In Vitro: 1 M HCl: 50 mg/mL (106.75 mM; Requires sonication) DMSO: 5 mg/mL (10.67 mM; Requires sonication and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| 1 M HCl | 50 mg/mL (106.75 mM) | requires sonication |
| DMSO | 5 mg/mL (10.67 mM) | requires sonication and adjust pH to 3 with HCl; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.34 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.34 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
Growth of C. neoformans, C. gattii, Candida albicans, and Aspergillus fumigatus was inhibited by Fosmanogepix (APX001) (2-0.002 μg/ml, 40-72 h), yielding MIC or minimum effective concentration (MEC) values of 0.008-0.25 μg/ml[1].
In Vivo
In a mouse cryptococcal meningitis (CM) model, Fosmanogepix (APX001) (390 mg/kg for Oral gavage, thrice daily) lowered the fungal burden[1]. Fosmanogepix (APX001) (100 mg/kg for Oral gavage) drives efficacy in CD-1 mice[1].
| Animal Model | murine model of cryptococcal meningitis[1] |
|---|---|
| Dosage | 390 mg/kg |
| Administration | Oral gavage (p.o.) |
| Result | Observed significant differences (P < 0.05) fungal burden and reduced the fungal burden compared to untreated control in the lung tissue. Reduced the fungal burden of 0.78 log10 CFU/g compared with control group in brain tissue. |
| Animal Model | CD-1 mice[1] |
|---|---|
| Dosage | 100 mg/kg |
| Administration | Intraperitoneal injection (i.p.) |
| Result | Extended the half-life of the active moiety, APX001A, from 1.3 to 8.8 h, resulting in a 9-fold increase in the area under the curve (AUC). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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