For research use only. Not for therapeutic Use.
Apratastat（Cat No.:I002604）is an orally active inhibitor of matrix metalloproteinases (MMPs) and tumor necrosis factor-alpha (TNF-α) converting enzyme (TACE), designed to reduce inflammation and tissue degradation. By inhibiting MMPs and TACE, apratastat helps regulate the breakdown of extracellular matrix proteins and reduces the release of pro-inflammatory cytokines, particularly TNF-α, which is crucial in inflammatory diseases. It has been investigated for potential use in conditions like rheumatoid arthritis, where excessive inflammation and tissue damage are key issues. Apratastat’s dual action makes it a promising candidate in chronic inflammatory and autoimmune disorder research.
| Catalog Number | I002604 |
| CAS Number | 287405-51-0 |
| Synonyms | TMI-005; TMI005; TMI 005;(3S)-N-Hydroxy-4-((4-((4-hydroxybut-2-ynyl)oxy)phenyl)sulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide |
| Molecular Formula | C17H22N2O6S2 |
| Purity | ≥95% |
| Target | tumour necrosis factor-α convertase inhibitor |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | (3S)-N-hydroxy-4-[4-(4-hydroxybut-2-ynoxy)phenyl]sulfonyl-2,2-dimethylthiomorpholine-3-carboxamide |
| InChI | InChI=1S/C17H22N2O6S2/c1-17(2)15(16(21)18-22)19(9-12-26-17)27(23,24)14-7-5-13(6-8-14)25-11-4-3-10-20/h5-8,15,20,22H,9-12H2,1-2H3,(H,18,21)/t15-/m0/s1 |
| InChIKey | MAVDNGWEBZTACC-HNNXBMFYSA-N |
| SMILES | CC1([C@@H](N(CCS1)S(=O)(=O)C2=CC=C(C=C2)OCC#CCO)C(=O)NO)C |
| Reference | </br>1:Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. Shu C, Zhou H, Afsharvand M, Duan L, Zhang H, Noveck R, Raible D.J Clin Pharmacol. 2011 Apr;51(4):472-81. doi: 10.1177/0091270010372389. Epub 2010 Nov 8. PMID: 21059888 </br>2:Drug evaluation: apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis. Thabet MM, Huizinga TW.Curr Opin Investig Drugs. 2006 Nov;7(11):1014-9. PMID: 17117591 |
