Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LX7101是 LIMK 和ROCK2高效抑制剂,对LIMK1/2、ROCK、PKA 的IC50分别为24、1.6、10 和小于1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 7,930 | 现货 | ||
50 mg | ¥ 10,300 | 6-8周 |
产品描述 | LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM). |
靶点活性 | ROCK2:10 nM, LIMK1:24 nM, PKA:1 nM, LIMK2:1.6 nM |
体外活性 | LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma. LX-7101 also shows effective inhibition of Akt1 (IC50<1 nM)[1]. The activity of LX7101 is primarily due to inhibition of LIMK2, under physiological conditions[2]. The overall selectivity of LX7101 for LIMK2 enhances the higher physiological ATP concentrations. |
体内活性 | Topical doses of LX-7101 are evaluated for tolerability in the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single-dose studies. LX-7101 is advanced to Phase-I clinical trials as intraocular pressure (IOP)-lowering agent for the treatment of glaucoma. LX-7101 shows a significant IOP reduction at time points ranging from 1 h to 6 h post-administration in rabbits[1]. LX-7101 (5%) achieved an additional reduction of IOP (5.0 mmHg total reduction) compared to the 0.1% formulation. It also demonstrated a long duration of action, in the mouse IOP assay, with IOP not returning to baseline until more than 8 h postdose[2]. |
分子量 | 451.52 |
分子式 | C23H29N7O3 |
CAS No. | 1192189-69-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (332.21 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL | 55.3685 mL |
5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | 11.0737 mL | |
10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL | 5.5369 mL | |
20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7684 mL | |
50 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1074 mL | |
100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5537 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。
LX7101 1192189-69-7 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells Tyrosine Kinase/Adaptors ROCK LIM Kinase PKA inhibit Inhibitor LX 7101 Rho-associated protein kinase LX-7101 Rho-associated kinase Rho-kinase ROK inhibitor