Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Marimastat (BB2516) 是一种血管生成和转移抑制剂,限制血管的生长和生成。它是一种广谱的,具有口服活性的MMPs 抑制剂,有效抑制 MMP-9 , MMP-1, MMP-2, MMP-14, MMP-7,用于癌症的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 628 | 现货 | ||
10 mg | ¥ 970 | 现货 | ||
25 mg | ¥ 1,780 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,220 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 692 | 现货 |
产品描述 | Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM). |
靶点活性 | MMP1:5 nM, MMP7:13 nM, MMP2:6 nM, MMP9:3 nM, MMP14:9 nM |
体外活性 | Marimastat (BB-2516) is a broad-spectrum MMPI with an enzyme inhibitory spectrum very similar to batimastat. [1] Marimastat inhibits CD30 shedding in Karpas 299 cells with an IC50 of 1 microM [2] and also inhibits LPS-induced soluble TNF-alpha production in a dose-dependent manner. The enzyme, tumor necrosis factor alpha convertase (TACE), reported to be closely related to matrix metalloproteinases, is responsible for the processing of pro-TNFalpha to TNFalpha and is specifically inhibited by Marimastat with an IC50 of 3.8 nM.[3] |
体内活性 | Marimastat has a favorable pharmacokinetic profile in humans, as it is almost completely absorbed after oral administration, with a high and predictable bioavailability and a half-life of approximately 15 hr (justifying twice a day dosing), making it a much more palatable treatment option for Clinicalal trials than batimastat. Marimastat is rapidly metabolized in rodents, undergoing a very high first-pass effect, making testing of marimastat in rodents difficult, as sustained plasma concentrations in this species are difficult to obtain. [1] |
激酶实验 | Compounds 1, 2, 7-9 and 11-16 are pre-incubated with MMP-1 or MMP-3 (10 nM) at different concentrations (0-10 μM) in a mixture of Tris-HCl (50 mM, pH 7.5), NaCl (150 mM), CaCl2 (10 mM), NaN3 (0.02%) and Brij-35 (0.05%) for 1 hour at 37°C. Residual activity is measured using the fluorogenic MMP substrate (2 μM) by fluorescence increase (emission at 393 nm and excitation at 325 nm) on a fluorescence plate reader. The data are fitted to the tight binding inhibitor equation: v=[(E-I-k+[(E-I-k)2+4Ek]1/2)/(2E)], where v is the velocity of the reaction, E is the enzyme concentration, I is the initial inhibitor concentration, and k is the apparent inhibition constant, using the software Prism. |
别名 | BB2516, 马立马司他, KB-R8898, TA2516 |
分子量 | 331.41 |
分子式 | C15H29N3O5 |
CAS No. | 154039-60-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.1 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.0174 mL | 15.0871 mL | 30.1741 mL | 75.4353 mL |
5 mM | 0.6035 mL | 3.0174 mL | 6.0348 mL | 15.0871 mL | |
10 mM | 0.3017 mL | 1.5087 mL | 3.0174 mL | 7.5435 mL | |
20 mM | 0.1509 mL | 0.7544 mL | 1.5087 mL | 3.7718 mL | |
50 mM | 0.0603 mL | 0.3017 mL | 0.6035 mL | 1.5087 mL | |
100 mM | 0.0302 mL | 0.1509 mL | 0.3017 mL | 0.7544 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Marimastat 154039-60-8 Proteases/Proteasome MMP BB-2516 KB-R 8898 TA 2516 inhibit BB2516 TA-2516 Inhibitor 马立马司他 KB-R8898 TA2516 BB 2516 KB-R-8898 Matrix metalloproteinases inhibitor