您好，欢迎来到试剂信息网！ [登录] [免费注册]
试剂信息网
发布求购
位置：首页 > 产品库 > SB-505124 hydrochloride
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
SB-505124 hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SB-505124 hydrochloride图片
CAS NO:356559-13-2
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
SB-505124 hydrochloride 是 TGF-β Receptor type I receptor (ALK4, ALK5, ALK7) 的选择性抑制剂，对 ALK4, ALK5 的 IC50 分别为 129 nM 和 47 nM，但不抑制 ALK1, 2, 3,或 6。
Cas No.356559-13-2
别名SB 505124 hydrochloride;SB505124 hydrochloride
化学名2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine
Canonical SMILESCC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4.Cl
分子式C20H22ClN3O2
分子量371.86
溶解度≥ 9.3 mg/mL in DMSO, ≥ 87 mg/mL in EtOH
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 value of 129 nM and 47 nM [1].

Anaplastic lymphoma kinase (ALK) gets involved in the development of the brain and influence specific neurons in the nervous system.

SB505124 is a reversible ATP competitive inhibitor of ALK4 and ALK5. Incubation of the ALK5 with high concentrations of SB505124, followed by dilution to a sub-IC50 concentration resulted in no effect of downstream Smad3 phosphorylation [2]. SB505124 was shown to have no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. Evidence showed that 100% drug will release within 12 h, and the gel showed no cytotoxicity to the cultured rabbit subconjunctival cells[2]. It was observed that ALK4 downstream effectors including pSmad2, CTGF, and α-SMA was inhibited by SB505124 in cultured fibroblasts [3].

In rabbit in glaucoma filtration surgery (GFS) model, the period of filtering blebs were reduced by TGFβ induced fibroblast. The filtering blebs in the GFS with SB505124 group were maintained for more than 10 days, and the period of bleb survival was significantly longer than that in controls, which suggested the significant inhibition of ALK4 and 5 by SB505124 [2]. It was observed that ALK4 downstream effectors CTGF and α-SMA were suppressed by SB-505124 in vivo[3].

References:
[1].  DaCosta B S et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol., 2004,65(3): 744-52.
[2].  Sutariya V, et al. Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol., 2013, 18(4): 957-962.
[3].  Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. Mol Vis., 2010, 16: 1880-1892.