APX-115 free base

APX-115, also known as EWHA-18278, is a potent, orally active pan NADPH oxidase (Nox) inhibitor. APX-115 protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. APX-115 might be a promising therapeutic agent for the treatment of DN because of its pan-NOX inhibitory activity, including its NOX5 inhibitory activity, and also owing to its anti-inflammatory effect.

Product information

CAS Number: 1270084-92-8

Molecular Weight: 279.34

Formula: C17H17N3O

Synonym:

EWHA-18278

EWHA18278

APX 115

APX-115 free base

APX115

EWHA 18278

Chemical Name: 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol

Smiles: CCCC1C(=NN(C=1O)C1=CC=CC=N1)C1C=CC=CC=1

InChiKey: LQKQLKMTJOMCMJ-UHFFFAOYSA-N

InChi: InChI=1S/C17H17N3O/c1-2-8-14-16(13-9-4-3-5-10-13)19-20(17(14)21)15-11-6-7-12-18-15/h3-7,9-12,21H,2,8H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

APX-115 free base (5 μM; 60 min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression in the mouse podocyte cell line. In the kidney, APX-115 free base attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes.

In Vivo:

APX-115 free base (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice. APX-115 free base treatment decreases the urinary excretion of albumin and plasma creatinine levels.

References:

1. Chocry M, Leloup L. The NADPH Oxidase Family and Its Inhibitors. Antioxid Redox Signal. 2020 Aug 10;33(5):332-353. doi: 10.1089/ars.2019.7915. Epub 2020 Jan 23. PMID: 31826639.
2. Dorotea D, Kwon G, Lee JH, Saunders E, Bae YS, Moon SH, Lee SJ, Cha DR, Ha H. A pan-NADPH Oxidase Inhibitor Ameliorates Kidney Injury in Type 1 Diabetic Rats. Pharmacology. 2018;102(3-4):180-189. doi: 10.1159/000491398. Epub 2018 Aug 10. PMID: 30099457.
3. Cha JJ, Min HS, Kim KT, Kim JE, Ghee JY, Kim HW, Lee JE, Han JY, Lee G, Ha HJ, Bae YS, Lee SR, Moon SH, Lee SC, Kim G, Kang YS, Cha DR. 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. doi: 10.1038/labinvest.2017.2. Epub 2017 Feb 6. PMID: 28165467.

Products are for research use only. Not for human use.