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Antiviral API
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ONX-0914
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| Category | Human immunodeficiency Virus (HIV) |
| CAS | 960374-59-8 |
| Description | ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome. Recent evidence suggests that the immunoproteasome regulates the production of several inflammatory cytokines, including Tumor Necrosis Factor-α (TNF-α), Interleukin-6 (IL-6), IL-17, and IL-23. In preclinical models of rhematoid arthritis and lupus, ONX 0914 blocked progression of these diseases at well-tolerated doses. Preclinical studies are underway to evaluate the potential of ONX 0914 in the treatment of a range of autoimmune disorders. |
Product Information
| Synonyms | ONX 0914; ONX0914; ONX-0914; PR957; PR-957; PR 957 |
| IUPAC Name | (2S)-3-(4-methoxyphenyl)-N-[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide |
| Molecular Weight | 580.6719 |
| Molecular Formula | C31H40N4O7 |
| Canonical SMILES | CC(C(=O)NC(CC1=CC=C(C=C1)OC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C)NC(=O)CN4CCOCC4 |
| InChI | InChI=1S/C31H40N4O7/c1-21(32-27(36)19-35-13-15-41-16-14-35)29(38)34-26(18-23-9-11-24(40-3)12-10-23)30(39)33-25(28(37)31(2)20-42-31)17-22-7-5-4-6-8-22/h4-12,21,25-26H,13-20H2,1-3H3,(H,32,36)(H,33,39)(H,34,38)/t21-,25-,26-,31+/m0/s1 |
| InChIKey | WQAVPPWWLLVGFK-VTNASVEKSA-N |
| Boiling Point | 878.0±65.0 °C at 760 mmHg |
| Flash Point | 484.8±34.3 °C |
| Purity | >98% |
| Density | 1.2±0.1 g/cm3 |
| Solubility | In vitro: 10 mM in DMSO |
| Appearance | white to off-white solid powder |
| Application | Proteasome Inhibitors |
| Storage | Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month |
| Complexity | 928 |
| Exact Mass | 580.28969963 |
| Index Of Refraction | 1.569 |
| In Vitro | ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation. |
| In Vivo | ONX-0914 (2-10 mg/kg; i.v,; on days 4, 6 and 8) meliorates disease in mouse arthritis ONX-0914 (2, 6 and 10 mg per kg body weight on days 25, 27, 29, 31 and 33; i.v.) treatment also induced a rapid therapeutic response in the T and B cell-dependent CIA (collagen-induced arthritis) model. |
| PSA | 149.07000 |
| Target | Proteasome; Bacterial; HIV |
| Vapor Pressure | 0.0±0.3 mmHg at 25°C |
| XLogP3-AA | 1.9 |
