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TMI 005
- Apratastat
- Optical Purity: >98% e.e.
- Soluble in DMSO
- MF: C17H22N2O6S2
- MW: 414.5
Description
TMI 005 is Apratastat, an orally active dual inhibitor of MMP13 and ADAM17, also known as TNF-α-converting enzyme (TACE). It reduces proteolytic release of soluble TNF-α and can modulate extracellular-matrix degradation.
The combined effects on inflammatory cytokine shedding and matrix-remodeling enzymes made TMI 005 a candidate disease-modifying agent for rheumatoid arthritis. It remains useful for studying ADAM17 biology, TNF-α processing and protease-driven joint tissue damage.
Key Features
- Orally active ADAM17/TACE inhibitor
- Reduces release of soluble TNF-α
- Also inhibits matrix metalloproteinase activity
- Links cytokine shedding to cartilage and bone remodeling
Applications
- ADAM17/TACE enzyme and substrate-shedding studies
- TNF-α processing and inflammatory signaling research
- Rheumatoid arthritis and joint-damage models
- Matrix metalloproteinase and extracellular-matrix remodeling studies
More Information
| Parent CAS No. | 287405-51-0 |
|---|---|
| Chemical Name | (S)-4-[4-(4-Hydroxy-but-2-ynyloxy)-benzenesulfonyl]-2,2-dimethyl-thiomorpholine-3-carboxylic acid hydroxyamide |
| SMILES | [C@@H]1(C(NO)=O)N(S(C2C=CC(OCC#CCO)=CC=2)(=O)=O)CCSC1(C)C |&1:0,r| |
| MFCD | N.A. |
| 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 |
| CID | 11452716 |
| Short Description | TACE/MMP inhibitor |
References
- MM Thabet and TWJ Huizinga. Apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis. Curr. Opin. Investig. Drugs. 2006, 7(11), 1014-1019.
- ML Moss et al. Drug Insight: Tumor Necrosis Factor Converting Enzyme as a Pharmaceutical Target for Rheumatoid Arthritis. Nat. Clin. Pract. Rheumatol. 2008, 4(6), 300.
- C Shu et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J. Clin. Pharmacol. 2011, 51(4), 472-481.
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