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.
| 説明 | 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. |
| In vitro | 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). |
| In vivo | 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 2 years
DMSO: 110 mg/mL (302.7 mM), Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
参考文献
投与量変換You can also refer to dose conversion for different animals. 詳細
In vivo投与量計算 (透明溶液)計算器bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
R-268712 879487-87-3 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors TGF-beta/Smad ALK renal fibrosis Thy1 nephritis Transforming growth factor beta receptors glomerulonephritis Transforming growth factor beta ALK tyrosine kinase receptor HFL-1 R 268712 glomerulosclerosis CD246 Inhibitor Cluster of differentiation 246 UUO Anaplastic lymphoma kinase (ALK) R268712 inhibit TGF-β CKD TGF-β Receptor Anaplastic lymphoma kinase inhibitor
