Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MMP13-IN-3 是口服有效的MMP-13选择性抑制剂,IC50为 1 nM,比其他 MMP 的选择性高 1000倍多。MMP13-IN-3在用于骨关节炎方面有研究的价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 786 | 现货 | ||
5 mg | ¥ 1,950 | 现货 | ||
10 mg | ¥ 3,130 | 现货 | ||
25 mg | ¥ 5,170 | 现货 | ||
50 mg | ¥ 7,320 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,990 | 现货 |
产品描述 | MMP13-IN-3 is >1000 selective over other MMPs. MMP13-IN-3 is an effective, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis. |
靶点活性 | MMP10:16 μM, MMP2:18 μM, MMP13:1 nM, MMP9:8.9 μM, MMP14:8.3 μM |
体外活性 | MMP13-IN-3 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC50s of 18, 8.9, 16 and 8.3 μM, respectively. MMP13-IN-3 is effective in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit the degradation of bovine nasal cartilage (IC50: 31 nM) [1]. |
体内活性 | MMP13-IN-3 has short terminal elimination half-life (t1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively). MMP13-IN-3 reaches micromolar plasma levels (AUC=1109±64 nM h/mL) when dosed orally at 10 mg/kg or i.v. 1 mg/kg. It displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The Vss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile [1]. |
分子量 | 446.46 |
分子式 | C24H22N4O5 |
CAS No. | 1222173-37-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (223.98 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2398 mL | 11.1992 mL | 22.3984 mL | 55.9961 mL |
5 mM | 0.448 mL | 2.2398 mL | 4.4797 mL | 11.1992 mL | |
10 mM | 0.224 mL | 1.1199 mL | 2.2398 mL | 5.5996 mL | |
20 mM | 0.112 mL | 0.56 mL | 1.1199 mL | 2.7998 mL | |
50 mM | 0.0448 mL | 0.224 mL | 0.448 mL | 1.1199 mL | |
100 mM | 0.0224 mL | 0.112 mL | 0.224 mL | 0.56 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。
MMP13-IN-3 1222173-37-6 Proteases/Proteasome MMP inhibit osteoarthritis Inhibitor MMP13 IN 3 Matrix metalloproteinases MMP-13-IN-3 MMP13IN3 MMP-13 inhibitor