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- CAS号:
154039-60-8
- 规格:
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥553.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥333.0 |
| 规格: | 5mg | 产品价格: | ¥502.0 |
| 规格: | 10mg | 产品价格: | ¥776.0 |
| 规格: | 25mg | 产品价格: | ¥1424.0 |
| 规格: | 50mg | 产品价格: | ¥2312.0 |
| 规格: | 100mg | 产品价格: | ¥3376.0 |
Product Introduction
Bioactivity
| 名称 | Marimastat |
| 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). |
| 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. |
| 体外活性 | Marimastat (BB-2516) 是一种具有广谱MMPI活性的化合物,其酶抑制谱与batimastat非常相似。Marimastat以1μM(IC50)抑制Karpas 299细胞中CD30的脱落,并且以剂量依赖的方式抑制LPS诱导的可溶性TNF-α产生。与基质金属蛋白酶紧密相关的酶,肿瘤坏死因子α转换酶(TACE),负责将前体TNFα处理成TNFα,Marimastat特异性地以3.8纳摩(IC50)抑制该酶。 |
| 体内活性 | Marimastat在人体中具有良好的药代动力学特性,口服给药后几乎完全吸收,具有高且可预测的生物利用度,半衰期约为15小时(说明每天两次给药是可行的),使其成为临床试验中比batimastat更受欢迎的治疗选择。Marimastat在啮齿动物体内迅速代谢,经历极高的首过效应,这使得在啮齿动物中测试Marimastat变得困难,因为在这种物种中难以获得持续的血浆浓度。[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.03 mM), Sonication is recommended. DMSO : 257.5 mg/mL (776.98 mM), Sonication is recommended. |
| 关键字 | TA-2516 | TA 2516 | MMP-9 | MMP-7 | MMP-2 | MMP-14 | MMP-1 | MMP | Matrix metalloproteinases | Marimastat | KB-R-8898 | KB-R 8898 | Inhibitor | inhibit | BB-2516 | BB 2516 |
| 相关产品 | Rhamnose monohydrate | Doxycycline (hyclate) | Astragaloside IV | Anethole | Meloxicam | Doxycycline | Glucosamine | Chloramphenicol | Methylchloroisothiazolinone/Methylisothiazolinone Mixture | Chondroitin sulfate | Propoxur | Edaravone |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Protease Inhibitor Library | Anti-Lung Cancer Compound Library | Immunology/Inflammation Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Cancer Drug Library |
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