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ARP-100 {[allProObj[0].p_purity_real_show]}

货号:A443997 同义名: CAY10609;MMP-2 Inhibitor III

ARP-100是一种选择性 MMP-2 抑制剂,IC50 为 12 nM,能够在体外显示抗侵袭特性,对其他 MMP 具有较低的抑制活性。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
ARP-100 化学结构 CAS号:704888-90-4
ARP-100 化学结构
CAS号:704888-90-4
ARP-100 3D分子结构
CAS号:704888-90-4
ARP-100 化学结构 CAS号:704888-90-4
ARP-100 3D分子结构 CAS号:704888-90-4
规格 价格 会员价 库存 数量
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ARP-100 纯度/质量文件 产品仅供科研

货号:A443997 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-14, IC50: 3 nM

MMP-7, IC50: 16 nM

98%
Ilomastat ++++

MMP-26, Ki: 0.36 nM

MMP-2, Ki: 0.1 nM

99%+
SB-3CT +

MMP-9, Ki: 600 nM

MMP-2, Ki: 13.9 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。

ARP-100 生物活性

描述 Matrix metalloproteinases (MMPs) are a family of zinc-dependent proteinases that are associated with the tumorigenic process. MMPs degrade the extracellular matrix, promoting tumor invasion and metastasis[1]. MMPs degrade various protein substrates in ECM including collagen and elastin. MMPs could also influence endothelial cell function as well as VSM cell migration, proliferation, Ca2+ signaling, and contraction. MMPs play a role in vascular tissue remodeling during various biological processes such as angiogenesis, embryogenesis, morphogenesis, and wound repair. Alterations in specific MMPs could influence arterial remodeling and lead to various pathological disorders such as hypertension, preeclampsia, atherosclerosis, aneurysm formation, as well as excessive venous dilation and lower extremity venous disease[2].ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1’pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM)[3].Inhibition of MMP activity with ARP-100 significantly improved the recovery of cardiac mechanical function and prevented the increase of a 70 kDa SERCA2a degradation fragment following IR injury, although 110 kDa SERCA2a and phospholamban levels appeared unchanged[4]. Significant increases in CD3, CD68, neutrophils, vascular cell adhesion molecule-1 and MMP-2 in perivascular adipose tissue(PVAT), and TGF-β1 and IMT of the aorta of TNF-α-injected mice were observed. PVAT of TNF-α-injected mice significantly up-regulated TGF-β1 and increased cell proliferation in a dose-dependent manner and was attenuated by SB-431542, batimastat, ARP 100 and TIMP-2[5].

ARP-100 参考文献

[1]Nithya Ramnath,et al. Matrix metalloproteinase inhibitors. Curr Oncol Rep. 2004 Mar;6(2):96-102.

[2]Xi Wang,et al. Matrix Metalloproteinases, Vascular Remodeling, and Vascular Disease. Adv Pharmacol. 2018;81:241-330.

[3] Rossello A, et al. New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg Med Chem. 2004 May 1;12(9):2441-50.

[4] Andrej Roczkowsky,et al. Myocardial MMP-2 contributes to SERCA2a proteolysis during cardiac ischaemia-reperfusion injury. Cardiovasc Res.2020 Apr 1;116(5):1021-1031.

[5]Kyaw Thu Moe,et al. Tumor necrosis factor-α induces aortic intima-media thickening via perivascular adipose tissue inflammation. J Vasc Res. 2013;50(3):228-37.

ARP-100 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL

ARP-100 技术信息

CAS号704888-90-4
分子式C17H20N2O5S
分子量 364.42
别名 CAY10609;MMP-2 Inhibitor III;​Matrix Metalloproteinase-2 Inhibitor III;Compound 10a
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解方案

DMSO: 105 mg/mL(288.13 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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