WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555871
Description: 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.
MedKoo Cat#: 555871
Name: APX-115 free base
Chemical Formula: C17H17N3O
Exact Mass: 279.1372
Molecular Weight: 279.343
Elemental Analysis: C, 73.10; H, 6.13; N, 15.04; O, 5.73
Synonym: APX-115 free base; APX 115; APX115; EWHA-18278; EWHA 18278; EWHA18278;
IUPAC/Chemical Name: 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol
InChi Key: LQKQLKMTJOMCMJ-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: OC1=C(CCC)C(C2=CC=CC=C2)=NN1C3=NC=CC=C3
NADPH oxidases (NOXs) are comprised of different isoforms, NOX1 to 5 and Duox1 and 2, and they trigger diabetic nephropathy (DN) in the patients with diabetes mellitus. Recently, it was shown that, compared to the other isoforms, the expression of NOX5 was increased in the patients with DN and, NOX5 has been suggested to be important in the development of therapeutic agents.
1: Lee ES, Kim HM, Lee SH, Ha KB, Bae YS, Lee SJ, Moon SH, Lee EY, Lee JH, Chung CH. APX-115, a pan-NADPH oxidase inhibitor, protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. Free Radic Biol Med. 2020 Oct 2;161:92-101. doi: 10.1016/j.freeradbiomed.2020.09.024. Epub ahead of print. PMID: 33011273.
2: 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.
3: 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.
4: Kwon G, Uddin MJ, Lee G, Jiang S, Cho A, Lee JH, Lee SR, Bae YS, Moon SH, Lee SJ, Cha DR, Ha H. 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. doi: 10.18632/oncotarget.18540. PMID: 29088780; PMCID: PMC5650335.
5: 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.