Powder: -20°C for 3 years | In solvent: -80°C for 1 year
R-268712 是选择性的 ALK5 抑制剂(IC50:2.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 378 | 现货 | ||
2 mg | ¥ 549 | 现货 | ||
5 mg | ¥ 892 | 现货 | ||
10 mg | ¥ 1,380 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 4,230 | 现货 | ||
100 mg | ¥ 5,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 981 | 现货 |
产品描述 | R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor. |
体外活性 | R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor.?Evaluation of in vitro inhibition indicated that R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). |
体内活性 | Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model.?Additionally, the efficacy of R-268712 in a heminephrectomized anti-Thy1 glomerulonephritis model at doses of 0.3 and 1mg/kg.?R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function. |
分子量 | 363.39 |
分子式 | C20H18FN5O |
CAS No. | 879487-87-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 110 mg/mL (302.7 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7519 mL | 13.7593 mL | 27.5186 mL | 68.7966 mL |
5 mM | 0.5504 mL | 2.7519 mL | 5.5037 mL | 13.7593 mL | |
10 mM | 0.2752 mL | 1.3759 mL | 2.7519 mL | 6.8797 mL | |
20 mM | 0.1376 mL | 0.688 mL | 1.3759 mL | 3.4398 mL | |
50 mM | 0.055 mL | 0.2752 mL | 0.5504 mL | 1.3759 mL | |
100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.688 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。
R-268712 879487-87-3 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad renal fibrosis Thy1 nephritis Transforming growth factor beta receptors glomerulonephritis Transforming growth factor beta ALK tyrosine kinase receptor HFL-1 glomerulosclerosis CD246 Inhibitor Cluster of differentiation 246 R 268712 UUO Anaplastic lymphoma kinase (ALK) inhibit TGF-β R268712 CKD TGF-β Receptor Anaplastic lymphoma kinase inhibitor