| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| A412540-5mg | 5mg | 3 | $147.90 | |
| A412540-10mg | 10mg | 3 | $246.90 | |
| A412540-25mg | 25mg | 2 | $494.90 | |
| A412540-50mg | 50mg | 2 | $741.90 |
TNF-α Selective Inhibitors | Activators | Antagonists
| Synonyms | 1-(pyridin-2-yl)-3-phenyl-4-propyl-1H-pyrazol-5-ol | 1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)- | APX115;APX 115;Ewha-18278;Ewha18278 | S0777 | Isuzinaxib | EWHA-18278 (free base) | APX-115 free base | 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazo |
|---|---|
| Specifications & Purity | Moligand™, ≥99% |
| Biochemical and Physiological Mechanisms | 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. APX-115 free base (Ewha-18278 free base) significantly suppresses |
| Storage Temp | Store at -20°C |
| Shipped In | Ice chest + Ice pads |
| Grade | Moligand™ |
| Product Description | Information APX-115 free base (Ewha-18278 free base) is a potent, orally active inhibitor ofpan NADPH oxidase (pan-Nox)with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules includingMCP-1/CCL2,IL-6, andTNFαin the diabetic kidney. Targets MCP-1/CCL2 ; IL-6 ; TNFα ; NOX2 (Cell-free assay); NOX4 (Cell-free assay) 33094,; 0.57 μM(Ki); 0.63 μM(Ki) |
| ALogP | 2.994 |
|---|---|
| HBD Count | 1 |
| Rotatable Bond | 4 |
| Pubchem Sid | 504771005 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504771005 |
| IUPAC Name | 5-phenyl-4-propyl-2-pyridin-2-yl-1H-pyrazol-3-one |
| 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/h3-7,9-12,19H,2,8H2,1H3 |
| InChi Key | GIWZEELPLKPYBA-UHFFFAOYSA-N |
| Canonical SMILES | CCCC1=C(NN(C1=O)C2=CC=CC=N2)C3=CC=CC=C3 |
| Isomeric SMILES | CCCC1=C(NN(C1=O)C2=CC=CC=N2)C3=CC=CC=C3 |
| PubChem CID | 51036475 |
| Molecular Weight | 279.34 |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
 H2218116 | Certificate of Analysis | Jun 08, 2022 | A412540 |
| H2218117 | Certificate of Analysis | Jun 08, 2022 | A412540 |
| H2218119 | Certificate of Analysis | Jun 08, 2022 | A412540 |
| H2218120 | Certificate of Analysis | Jun 08, 2022 | A412540 |
| 1. Cha JJ, Min HS, Kim KT, Kim JE, Ghee JY, Kim HW, Lee JE, Han JY, Lee G, Ha HJ et al.. (2017) APX-115, a first-in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury.. Lab Invest, 97 (4): (419-431). [PMID:28165467] [10.1021/op500134e] |
| 2. Kwon G, Uddin MJ, Lee G, Jiang S, Cho A, Lee JH, Lee SR, Bae YS, Moon SH, Lee SJ et al.. (2017) A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced diabetic mice: possible role of peroxisomal and mitochondrial biogenesis.. Oncotarget, 8 (43): (74217-74232). [PMID:29088780] [10.1021/op500134e] |
| 3. Dorotea D, Kwon G, Lee JH, Saunders E, Bae YS, Moon SH, Lee SJ, Cha DR, Ha H. (2018) A pan-NADPH Oxidase Inhibitor Ameliorates Kidney Injury in Type 1 Diabetic Rats.. Pharmacology, 102 (3-4): (180-189). [PMID:30099457] [10.1021/op500134e] |
| 4. Lee ES, Kim HM, Lee SH, Ha KB, Bae YS, Lee SJ, Moon SH, Lee EY, Lee JH, Chung CH. (2020) APX-115, a pan-NADPH oxidase inhibitor, protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice.. Free Radic Biol Med, 161 (13): (92-101). [PMID:33011273] [10.1021/op500134e] |
| 5. Chocry M, Leloup L. (2020) The NADPH Oxidase Family and Its Inhibitors.. Antioxid Redox Signal, 33 (5): (332-353). [PMID:31826639] [10.1021/op500134e] |
