| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H21ClN4O4 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
EDI048 is an orally active, gut-restricted parasiticidal agent that binds specifically to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocking parasite membrane biogenesis, arresting the pathogen at the schizont stage, and thereby irreversibly clearing the infection. It is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, giving extremely low systemic exposure, a good safety profile, and no cardiotoxicity, genotoxicity or off-target effects, and it has been used in studies of intestinal cryptosporidiosis in children[1]. It is supplied as a light yellow to yellow solid (C25H21ClN4O4, MW 476.91) at 99.86% purity.
Physical & Chemical Properties
| CAS Number | 2767264-57-1 |
|---|---|
| Molecular Formula | C25H21ClN4O4 |
| Molecular Weight | 476.91 g/mol |
| Purity | 99.86% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C(C1=CC(N(C)C(C2=CC3=C(C4=CC=C(C(NC)=O)C=C4)C=NN3C=C2)=O)=CC=C1Cl)OC |
| Signaling Pathway | PI3K/Akt/mTOR; Anti-infection |
| Solubility | In Vitro: DMSO: 100 mg/mL (209.68 mM; Requires sonication; 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, 6 months; -20°C, 1 month. |
| 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 |
|---|---|---|
| DMSO | 100 mg/mL (209.68 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); 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 (5.24 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. |
Data provided by the manufacturer.
In Vitro
After 5 min preincubation + 50 min incubation, EDI048 (1 nM-20 μM) potently blocks wild-type Cryptosporidium parvum PI(4)K, with an IC50 of 0.004 μM; this activity relies on conserved tyrosines Y705 and Y907 located in the ATP-binding pocket of the enzyme[1]. In HCT-8 cell cultures, the asexual life cycle of Cryptosporidium parvum (48 h EC50=0.052 μM) and that of Cryptosporidium hominis (48 h EC50=0.050 μM) are potently inhibited by EDI048[1]. EDI048 (27 nM-20 μM; 72 h) shows antiparasitic activity against Cryptosporidium parvum in HCT-8 cell cultures. Maximal parasite clearance (clearance rate >99%) is reached with EDI048 at concentrations ≥27 nM, and the clearance half-life is approximately 15 h[1]. In HCT-8 cell cultures, EDI048 (3× EC50; 4 h) has irreversible parasiticidal activity at the merozoite maturation stage (8-12 h post-infection) of Cryptosporidium parvum, but does not affect growth at the early trophozoite stage[1].
Cell Viability Assay[1]
| Cell Line | HCT-8 human ileocaecal colorectal adenocarcinoma cells infected with Cryptosporidium parvum or Cryptosporidium hominis |
|---|---|
| Concentration | 10-point 3-fold serial dilutions |
| Incubation Time | 48 h (starting at 3 h post-infection) |
| Result | Inhibited Cryptosporidium parvum with an EC50 of 0.052 μM. Inhibited Cryptosporidium hominis with an EC50 of 0.050 μM. |
In Vivo
In immunocompromised mice infected with cryptosporidiosis, EDI048 (1-10 mg/kg; p.o.; once daily; for 5 consecutive days) is efficacious in a dose-dependent manner while systemic exposure stays extremely low[1]. In neonatal calves infected with cryptosporidiosis, EDI048 (10 mg/kg; p.o.; every 12 hours; for 7 consecutive days) significantly lowers fecal oocyst excretion and quickly relieves diarrhea symptoms, and infection does not recur after treatment[1].
| Animal Model | B6.129S7-Ifngtm1Ts/J (female, 6-8 weeks old, IFN-γ-knockout)[1] |
|---|---|
| Dosage | 1 mg/kg; 3 mg/kg; 10 mg/kg |
| Administration | p.o.; daily; 5 days |
| Result | Achieved a 0.3 log reduction in faecal oocyst shedding. Achieved a 1.1 log reduction in faecal oocyst shedding. Achieved a 3.1 log reduction in faecal oocyst shedding. Resulted in undetectable systemic exposure at 1 mg/kg and 3 mg/kg. Reached a maximum serum concentration (Cmax) of 8.4 nM and area under the curve (AUC) of 20.4 nM·h at 10 mg/kg. |
| Animal Model | Holstein-Friesian (neonatal bull and heifer, ≥30 kg birth weight)[1] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | p.o.; every 12 hours; 7 days |
| Result | Reduced faecal oocyst shedding significantly compared to untreated controls. Improved faecal consistency scores compared to untreated controls. Resolved diarrhoea by 48 hours post-treatment. Reduced days of severe diarrhoea and moderate-to-severe diarrhoea compared to controls. Prevented infection recrudescence for 7 days after treatment cessation. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Development of a Luciferase-Based In Vitro Assay to Evaluate the Efficacy of Anti-Cryptosporidial Drugs Against Cryptosporidium parvum. Pharmaceuticals (Basel) 2026 Apr 3;19(4):576. PMID: 42075832
