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CL-82198

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Chemical Structure| 307002-71-7 同义名 : -
CAS号 : 307002-71-7
货号 : A529182
分子式 : C17H22N2O3
纯度 : 98%
分子量 : 302.368
MDL号 : MFCD12828877
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(347.26 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Matrix metalloproteinases (MMPs) such as MMP13 promote tumour growth and progression by mediating extracellular matrix (ECM) reorganization and regulating the biological activity of cytokines[3]. MMP13 is a vital component for chondrocyte and osteoblast maturation, and is aberrantly expressed in numerous disease states. At the transcriptional level, MMP13 is controlled by many different growth factors and hormones. Most notably, MMP13 is regulated by the vitamin D hormone (1,25(OH)2D3), parathyroid hormone (PTH), and several cytokines[4]. 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[5]. CL-82198 (10 μM; 24 hours) significantly reduces LS174 cell migration[6]. CL-82198 decreases CTGF and TGF-β1 protein levels in hepatic stellate cells[7]. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression. CL82198 (1-10 mg/kg; i.p.; every other day for 12 weeks) prevents and decelerates MLI-induced osteoarthritis progression[8].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.54mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL
参考文献

[1]Wohlauer M, Moore EE, 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.

[2]Rath T, Stockle J, 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.

[3] Wiltrud Lederle,et al. MMP13 as a stromal mediator in controlling persistent angiogenesis in skin carcinoma. Carcinogenesis. 2010 Jul;31(7):1175-84.

[4]Mark B Meyer,et al. Selective regulation of Mmp13 by 1,25(OH) 2 D 3, PTH, and Osterix through distal enhancers. J Steroid Biochem Mol Biol. 2016 Nov;164:258-264.

[5] 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.

[6]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.

[7] 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.

[8] Wang M,et al. MMP13 is a critical target gene during the progression of osteoarthritis. Arthritis Res Ther. 2013 Jan 8;15(1):R5.