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Isuzinaxib (APX-115 free base) NADPH-oxidase inhibitor

Cat.No.S0777

Isuzinaxib (APX-115 free base, Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. This compound significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
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Quality Control

Batch: Purity: 99.05%
99.05

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (200.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 279.34 Formula

C17H17N3O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1270084-92-8 -- Storage of Stock Solutions

Synonyms Ewha-18278 free base SMILES CCCC1=C(NN(C1=O)C2=CC=CC=N2)C3=CC=CC=C3

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
MCP-1/CCL2
IL-6
TNFα
NOX2
(Cell-free assay)
0.57 μM(Ki)
NOX4
(Cell-free assay)
0.63 μM(Ki)
NOX1
(Cell-free assay)
1.08 μM(Ki)
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-07-18)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06962098 RECRUITING
Diabetic Kidney Disease (DKD)
Aptabio Therapeutics, Inc.
2025-05-26 PHASE2
NCT05758896 COMPLETED
Contrast Induced Acute Kidney Injury
Aptabio Therapeutics, Inc.
2023-12-27 PHASE2
NCT04534439 Completed
Diabetic Nephropathies|Diabetes Mellitus Type 2|Nephropathy Diabetic
Aptabio Therapeutics Inc.
2020-08-24 Phase 2

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