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Prinomastat

产品编号 T12539L CAS 192329-42-3

别名: KB-R9896, 普啉司他, AG3340

Prinomastat inhibits MMP-2, MMP-3 and MMP-9 (Kis: 0.05 nM, 0.3 nM and 0.26 nM, respectively). Prinomastat crosses the blood-brain barrier. It also has antitumor activity. Prinomastat is a broad-spectrum, potent, orally active metalloproteinase inhibitor (IC50s of 79, 6.3, and 5.0 nM for MMP-1, MMP-3, and MMP-9, respectively).

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Prinomastat, CAS 192329-42-3

规格	价格/CNY	货期
1 mg	￥ 525	35日内发货
5 mg	￥ 2,200	35日内发货
10 mg	￥ 4,140	35日内发货
25 mg	￥ 8,410	35日内发货

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其他形式的 Prinomastat:

Prinomastat hydrochloride
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Prinomastat inhibits MMP-2, MMP-3 and MMP-9 (Kis: 0.05 nM, 0.3 nM and 0.26 nM, respectively). Prinomastat crosses the blood-brain barrier. It also has antitumor activity. Prinomastat is a broad-spectrum, potent, orally active metalloproteinase inhibitor (IC50s of 79, 6.3, and 5.0 nM for MMP-1, MMP-3, and MMP-9, respectively).
靶点活性	MMP1:79 nM, MMP2:0.05 nM （ki）, MMP9:0.26 nM （ki）, MMP9:5 nM, MMP3:0.3 nM （ki）, MMP3:6..3 nM
体外活性	In C57MG/Wnt1 cells, the effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat. Prinomastat (0.1-1 μg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat. Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. The migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells [1].
体内活性	Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition (a short T1/2: 1.6 hours). The mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumor inoculation in a human fibrosarcoma mouse model (HT1080) [1].

别名	KB-R9896, 普啉司他, AG3340
分子量	423.51
分子式	C18H21N3O5S2
CAS No.	192329-42-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Sørensen MD, et al. Cyclic phosphinamides and phosphonamides, novel series of potent matrix metalloproteinase inhibitors with antitumour activity. Bioorg Med Chem. 2003 Dec 1;11(24):5461-84. 2. Blavier L, et al. Stromelysin-1 (MMP-3) is a target and a regulator of Wnt1-induced epithelial-mesenchymal transition (EMT). Cancer Biol Ther. 2010 Jul 15;10(2):198-208. 3. Shalinsky DR, et al. Broad antitumor and antiangiogenic activities of AG3340, a potent and selective MMP inhibitor undergoing advanced oncology clinical trials. Ann N Y Acad Sci. 1999 Jun 30;878:236-70. 4. Ozerdem U, et al. The effect of prinomastat (AG3340), a potent inhibitor of matrix metalloproteinases, on a subacute model of proliferative vitreoretinopathy. Curr Eye Res. 2000 Jun;20(6):447-53.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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