Powder: -20°C for 3 years | In solvent: -80°C for 1 year
T-26c 是高效的、选择性的基质金属蛋白酶-13 抑制剂,IC50=6.75 pM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
2 mg | ¥ 598 | 现货 | ||
5 mg | ¥ 970 | 现货 | ||
10 mg | ¥ 1,690 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | ¥ 4,960 | 现货 | ||
100 mg | ¥ 6,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,050 | 现货 |
产品描述 | T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor (IC50: 6.75 pM). |
靶点活性 | MMP13:6.75 pM (cell free) |
体外活性 | T-26c was the highly potent and selective MMP13 inhibitor with an IC50 value of 6.9 pM and more than 2600-fold selectivity over the other related metalloenzymes. Furthermore, the inhibitor was shown to be active in bovine nasal cartilage explants assay. T-26c significantly inhibited the breakdown of collagen (87.4% inhibition at 0.1 μM) in IL-1b and oncostatin M stimulated cartilage. |
体内活性 | Oral administration of the disodium salt formulations of T-26c to guinea pigs resulted in significant increases in AUC (8357 ng·h/mL) and Cmax (1445 ng/mL) compared with those of the free acid T-26c (AUC = 6478 ng·h/mL and Cmax = 911 ng/mL). The compound was well absorbed in all species at the oral dose of 10–20 mg/kg. |
激酶实验 | The MMP assay buffer consisted of 50 mM Tris–HCl (pH 7.5), 10 mM CaCl2, 150 mM NaCl, and 0.05% Brij-35. The pro-MMPs were activated by preincubation with 1 mM aminophenylmercuric acetate (APMA) in assay buffer at 37 °C for 2 h (MMP-1, 2, 7, 8, 10, and 13) or 18 h (MMP-3 and 9). The TACE assay buffer consisted of 25 mM Tris–HCl (pH 9.0), 2.5 mM ZnCl2, and 0.005% Brij-35. The pro-MMPs were activated by preincubation with 1 mM aminophenylmercuric acetate (APMA) in assay buffer at 37 °C for 2 h (MMP-1, 2, 7, 8, 10, and 13) or 18 h (MMP-3 and 9). Enzyme inhibition assays were performed in an assay buffer containing enzymes and fluorescence peptide (Cy3-PLGLK(Cy5Q)AR-NH2 for MMPs, Cy3-PLAQAV(Cy5QL-2,3-diaminopropionic acid)-RSSSR-NH2 for TACE) in the presence of the various concentrations of inhibitors. Following incubation at 37 °C for 40 min, the reaction was terminated by addition of EDTA (pH 8.0). The increase in fluorescence as measured by Farcyte spectrofluorimeter. Enzyme activity (%) was determined as following equation: Enzyme activity (%) = (X - C)/(T - C) × 100, where X = the fluorescence count with inhibitor, T = the fluorescence count without inhibitor and C = the fluorescence count with EDTA. IC50 values of inhibitors were obtained with iterative fitting package. |
细胞实验 | Bovine nasal septum cartilage was sliced, and the slices were maintained in the medium of a 1:1 (v/v) mixture of Dulbecco's modified Eagle's MEM and Ham's F-12 medium (DMEM/F-12) containing 10 % fetal calf serum overnight. After confirming that the slices were not contaminated, they were cultured in DMEM/F-12 medium containing 20 μg/mL gentamycin, 50 μg/mL streptomycin, and 50 U/mL penicillin (culture medium) for 2 days at 37 °C. The cartilage slices were cut into small cubes (ca. 1mm3) and transferred individually into wells of a 96 well plate with 100 μL of culture medium. For the collagen degradation assay, the medium was supplemented with 10 ng/mL IL-1β and 50 ng/mL oncostatin M in the presence or absence of compounds. The cartilage was incubated for 2 weeks. The supernatants were harvested and replaced with fresh medium containing identical test compounds every 7 days. Supernatants of day 7 and day 14 were collected and stored at -20 °C until assay. At the end of the culture, the remaining cartilage was completely digested with papain. Hydroxyproline release in the media from each explant was determined as a measure of collagen degradation by use of chloramine T and p-dimethylaminobenzaldehyde. The percentage of inhibitory activity against collagen degradation was calculated as follows: % of inhibition = [(% of collagen degradation with IL-1b and OSM) - (% of collagen degradation with IL-1β, OSM, and test sample)]/[(% of collagen degradation with IL-1β and OSM) - (% of collagen degradation without additives)] × 100. |
分子量 | 479.51 |
分子式 | C24H21N3O6S |
CAS No. | 869296-13-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (25.03 mM)
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0855 mL | 10.4273 mL | 20.8546 mL | 52.1366 mL |
5 mM | 0.4171 mL | 2.0855 mL | 4.1709 mL | 10.4273 mL | |
10 mM | 0.2085 mL | 1.0427 mL | 2.0855 mL | 5.2137 mL | |
20 mM | 0.1043 mL | 0.5214 mL | 1.0427 mL | 2.6068 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。
T-26c 869296-13-9 Proteases/Proteasome MMP T26c Inhibitor Matrix metalloproteinases T 26c inhibit inhibitor