2. PI3K/Akt/mTOR Anti-infection
  3. PI4K Parasite
  4. EDI048

EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children.

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EDI048

EDI048 Chemical Structure

CAS No. : 2767264-57-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

EDI048 Related Antibodies

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Description

EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children[1].
In Vitro

EDI048 (1 nM-20 μM; 5 min preincubation + 50 min incubation) potently inhibits wild-type Cryptosporidium parvum PI(4)K with an IC50 of 0.004 μM, and its activity depends on the conserved tyrosine residues Y705 and Y907 in the ATP-binding pocket of this enzyme[1].
EDI048 potently inhibits the asexual life cycles of Cryptosporidium parvum (48 h EC50=0.052 μM) and Cryptosporidium hominis (48 h EC50=0.050 μM) in HCT-8 cell cultures[1].
EDI048 (27 nM-20 μM; 72 h) exhibits antiparasitic activity against Cryptosporidium parvum in HCT-8 cell cultures. EDI048 achieves maximal parasite clearance (clearance rate >99%) at concentrations ≥27 nM, with a clearance half-life of approximately 15 h[1].
EDI048 (3× EC50; 4 h) exerts irreversible parasiticidal activity against Cryptosporidium parvum at the merozoite maturation stage (8-12 h post-infection) in HCT-8 cell cultures, but has no effect on the growth of the early trophozoite stage[1].

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

EDI048 Related Antibodies

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

EDI048 (1-10 mg/kg; p.o.; once daily; for 5 consecutive days) exhibits dose-dependent efficacy in immunocompromised mice infected with cryptosporidiosis, with extremely low systemic exposure[1].
EDI048 (10 mg/kg; p.o.; once every 12 hours; for 7 consecutive days) significantly reduces fecal oocyst excretion and rapidly alleviates diarrhea symptoms in neonatal calves infected with cryptosporidiosis, with no recurrence of infection after treatment[1].

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

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.
Clinical Trial
Molecular Weight

476.91

Formula

C25H21ClN4O4
CAS No.
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
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 (209.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0968 mL 10.4842 mL 20.9683 mL
5 mM 0.4194 mL 2.0968 mL 4.1937 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.86%

SDS (251 KB)

COA (251 KB) HNMR (280 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0968 mL 10.4842 mL 20.9683 mL 52.4208 mL
5 mM 0.4194 mL 2.0968 mL 4.1937 mL 10.4842 mL
10 mM 0.2097 mL 1.0484 mL 2.0968 mL 5.2421 mL
15 mM 0.1398 mL 0.6989 mL 1.3979 mL 3.4947 mL
20 mM 0.1048 mL 0.5242 mL 1.0484 mL 2.6210 mL
25 mM 0.0839 mL 0.4194 mL 0.8387 mL 2.0968 mL
30 mM 0.0699 mL 0.3495 mL 0.6989 mL 1.7474 mL
40 mM 0.0524 mL 0.2621 mL 0.5242 mL 1.3105 mL
50 mM 0.0419 mL 0.2097 mL 0.4194 mL 1.0484 mL
60 mM 0.0349 mL 0.1747 mL 0.3495 mL 0.8737 mL
80 mM 0.0262 mL 0.1311 mL 0.2621 mL 0.6553 mL
100 mM 0.0210 mL 0.1048 mL 0.2097 mL 0.5242 mL
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EDI048 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

EDI0482767264-57-1EDI 048EDI-048PI4KParasitePhosphatidylinositol 4 kinasesPI4 kinasesmeront stagemerozoiteCryptosporidium phosphatidylinositol-4-OH kinaseCryptosporidium parvumpaediatric enteric cryptosporidiosisHCT-8 cell culturesCryptosporidiumprimary hepatocytesCpPI(4)KCryptosporidium hominisInhibitorinhibitorinhibit

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