| Bioactivity | CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs[1][2]. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression[4]. | ||||||||||||
| Invitro | CL-82198 (10 μM; 24 hours) significantly reduces LS174 cell migration[1].CL-82198 decreases CTGF and TGF-β1 protein levels in hepatic stellate cells[3]. | ||||||||||||
| In Vivo | CL82198 (1-10 mg/kg; i.p.; every other day for 12 weeks) prevents and decelerates MLI-induced osteoarthritis progression[4]. Animal Model: | ||||||||||||
| Name | CL-82198 | ||||||||||||
| CAS | 307002-71-7 | ||||||||||||
| Formula | C17H22N2O3 | ||||||||||||
| Molar Mass | 302.37 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Rath T et al. Matrix metalloproteinase-13 is regulated by toll-like receptor-9 in colorectal cancer cells and mediates cellular migration. Oncol Lett. 2011 May;2(3):483-488. [2]. George J, et al. MMP-13 deletion decreases profibrogenic molecules and attenuates N-nitrosodimethylamine-induced liver injury and fibrosis in mice. J Cell Mol Med. 2017 Dec;21(12):3821-3835. [3]. Wohlauer M et al. Nebulized hypertonic saline attenuates acute lung injury following trauma and hemorrhagic shock via inhibition of matrix metalloproteinase-13. Crit Care Med. 2012 Sep;40(9):2647-53. [4]. Wang M,et al. MMP13 is a critical target gene during the progression of osteoarthritis. Arthritis Res Ther. 2013 Jan 8;15(1):R5. |