| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
EZ-482 targets apolipoprotein E (apoE), specifically binding to the C-terminal domain of both apoE3 and apoE4 isoforms. It binds to apoE4 through a unique N-terminal allostery. The compound is being studied for its potential to modulate apoE function in Alzheimer's disease.
|
|---|---|
| ln Vitro |
The C-terminal domain of EZ-482 contains residues 229–243 and 258–265 that bind to the apoE site [1]. Boiling heparin binding in a concentrated form is called EZ-482 (0.5, 1, 5, 10 μM; 1 hour) [1].
In vitro, EZ-482 blocks heparin binding to apoE in a concentration-dependent manner at concentrations of 0.5, 1, 5, and 10 μM. It binds to the C-terminal domain of apoE3 and apoE4 with a Kd of 5-10 μM. The compound's binding to apoE4 occurs through a unique N-terminal allosteric effect. |
| ln Vivo |
In vivo activity data for EZ-482 are not extensively documented in publicly available literature. As a research tool for Alzheimer's disease, EZ-482 is expected to modulate apoE function in animal models of neurodegeneration. Further in vivo studies are needed to fully characterize its pharmacological effects and therapeutic potential in cognitive impairment models.
|
| Enzyme Assay |
The in vitro binding assay for EZ-482 typically involves surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure its affinity for recombinant apoE3 and apoE4 proteins. Binding is assessed by incubating varying concentrations of EZ-482 with immobilized apoE protein, and the dissociation constant (Kd) is calculated. EZ-482 binds to the C-terminal domain of apoE3 and apoE4 with a Kd of 5-10 μM.
|
| Cell Assay |
In vitro cellular assays for EZ-482 typically involve treating cultured neuronal or glial cell lines expressing apoE isoforms. Heparin binding assays are performed to assess the compound's ability to block apoE-heparin interactions in a concentration-dependent manner at 0.5, 1, 5, and 10 μM. Cell viability and apoE-mediated signaling pathways may also be evaluated.
|
| Animal Protocol |
In vivo animal experiments for EZ-482 would typically use transgenic mouse models of Alzheimer's disease expressing human apoE isoforms. The compound would be administered via appropriate routes (e.g., oral, intraperitoneal) at various doses. Cognitive function would be assessed using behavioral tests such as the Morris water maze. Brain levels of apoE and amyloid-beta pathology would be evaluated post-mortem. However, specific in vivo protocols for EZ-482 are not well documented in public literature.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of EZ-482 have not been extensively characterized in publicly available literature. As a small molecule with molecular weight of 501.9 (C23H19ClN4O5S), EZ-482 is expected to have moderate oral bioavailability and reasonable blood-brain barrier penetration. Further PK studies including absorption, distribution, metabolism, and excretion are needed to fully characterize its pharmacokinetic profile.
|
| Toxicity/Toxicokinetics |
Toxicological (toxicology) data for EZ-482 are limited in publicly available sources. The compound is described as having low off-target toxicity based on its selective binding to apoE. However, systematic toxicology studies including acute toxicity, repeated-dose toxicity, genotoxicity, and reproductive toxicity have not been well documented. Standard safety pharmacology studies would be required for full toxicological characterization.
|
| References |
[1]. Tridib Mondal, et al. ApoE: In Vitro Studies of a Small Molecule Effector. Biochemistry. 2016 May 10;55(18):2613-21.
|
| Additional Infomation |
EZ-482 (CAS#: 1016456-76-0) is a research compound being investigated for Alzheimer's disease. Its mechanism of action involves binding to apolipoprotein E (apoE) through a unique N-terminal allosteric effect. The compound is not approved for clinical use and remains an investigational tool for studying apoE biology and neurodegenerative diseases. No clinical trials have been registered for EZ-482 to date.
|
| Molecular Formula |
C23H19CLN4O5S
|
|---|---|
| Molecular Weight |
498.938762903214
|
| Exact Mass |
498.076
|
| CAS # |
1016456-76-0
|
| PubChem CID |
24673104
|
| Appearance |
White to off-white solid powder
|
| LogP |
3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
34
|
| Complexity |
908
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CLWDCBBEVQRZLY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H19ClN4O5S/c1-28-23(31)18-8-3-2-7-17(18)19(26-28)13-22(30)25-20-12-16(9-10-21(20)29)34(32,33)27-15-6-4-5-14(24)11-15/h2-12,27,29H,13H2,1H3,(H,25,30)
|
| Chemical Name |
N-[5-[(3-chlorophenyl)sulfamoyl]-2-hydroxyphenyl]-2-(3-methyl-4-oxophthalazin-1-yl)acetamide
|
| Synonyms |
EZ 482; EZ482; EZ-482
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~167.01 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0042 mL | 10.0212 mL | 20.0425 mL | |
| 5 mM | 0.4008 mL | 2.0042 mL | 4.0085 mL | |
| 10 mM | 0.2004 mL | 1.0021 mL | 2.0042 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
