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CL-82198 {[allProObj[0].p_purity_real_show]}

货号:A529182

CL-82198是一种选择性的 MMP-13 抑制剂,可用于骨关节炎 (OA) 的研究。

CL-82198 化学结构 CAS号:307002-71-7
CL-82198 化学结构
CAS号:307002-71-7
CL-82198 3D分子结构
CAS号:307002-71-7
CL-82198 化学结构 CAS号:307002-71-7
CL-82198 3D分子结构 CAS号:307002-71-7
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CL-82198 纯度/质量文件 产品仅供科研

货号:A529182 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 MMP 其他靶点 纯度
Marimastat +++

MMP-7, IC50: 16 nM

MMP-14, IC50: 3 nM

98%
Ilomastat ++++

MMP-2, Ki: 0.1 nM

MMP-26, Ki: 0.36 nM

99%+
SB-3CT +

MMP-2, Ki: 13.9 nM

MMP-9, Ki: 600 nM

99%+
Doxycycline 98%
NSC 405020 98%
Batimastat +++

MMP-1, IC50: 3 nM

MMP-7, IC50: 4 nM

99%+
Nobiletin 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

CL-82198 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].

CL-82198 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.

CL-82198 实验方案

计算器
存储液制备 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

CL-82198 技术信息

CAS号307002-71-7
分子式C17H22N2O3
分子量 302.368
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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