[CAS NO. 1395946-75-4] APX-115
PRODUCTS SPECIFICATIONS [1395946-75-4]
DESCRIPTION [1395946-75-4]
Overview
| MDL | MFCD32201051 |
|---|---|
| Molecular Weight | 315.80 |
| Molecular Formula | C17H18ClN3O |
| SMILES | OC1=C(CCC)C(C2=CC=CC=C2)=NN1C3=NC=CC=C3.Cl |
1 Publications Citing Use of MCE
Summary
APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K i values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1 , Nox2 and Nox4 , respectively. APX-115 effectively prevents kidney injury [1] .
IC50 & Target
Ki: 1.08 μM (Nox1), 0.57 μM (Nox2) and 0.63 μM (Nox4) [1]
In Vitro
APX-115 (5 μM; 60 min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression in the mouse podocyte cell line
[2]
.
In the kidney, APX-115 attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
APX-115 (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice
[2]
.
APX-115 treatment decreases the urinary excretion of albumin and plasma creatinine levels
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db ) [2] |
| Dosage: | 60 mg/kg |
| Administration: | Oral gavage; per day; for 12 weeks |
| Result: | Significantly improved insulin resistance in diabetic mice. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04534439 | Aptabio Therapeutics, Inc. |
Diabetic Nephropathies|Diabetes Mellitus, Type 2|Nephropathy, Diabetic
|
August 24, 2020 | Phase 2 |
| NCT03694041 | Aptabio Therapeutics, Inc. |
Healthy|Safety
|
May 28, 2018 | Phase 1 |
| NCT04880109 | Aptabio Therapeutics, Inc.|Covance |
COVID-19
|
October 20, 2021 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 316.66 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 mL |
References
- [1] Kwon G, et al. A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced diabetic mice: possible role of peroxisomal and mitochondrial biogenesis. Oncotarget. 2017 Jun 16;8(43):74217-74232.
- [2] Cha JJ, et al. APX-115, a first-in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury. Lab Invest. 2017 Apr;97(4):419-431.
