您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > A 205804
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：
 
A 205804
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。
A 205804图片
CAS NO:251992-66-2
包装与价格：
包装价格(元)
10mg电议
50mg电议
500mg电议
1g电议

产品介绍
A 205804 是一种可口服的、有效的、选择性的 E-selectin 和 ICAM-1 表达的先导抑制剂，对 E-selectin 和 ICAM-1 的 IC50 分别为 20 nM 和 25 nM。
Cas No.251992-66-2
别名4-[(4-甲基苯基)硫基]噻吩并[2,3-C]吡啶-2-甲酰胺
化学名4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide
Canonical SMILESCC1=CC=C(C=C1)SC2=C3C=C(SC3=CN=C2)C(=O)N
分子式C15H12N2OS2
分子量300.39
溶解度≥ 30mg/mL in DMSO
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

A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 value of 20 nM and 25 nM, respectively [1].

E-selectin is a cell adhesion molecule and plays an important role in recruiting leukocytes to injury site during inflammation process. ICAM-1 (intracellular adhesion molecule 1) is a ligand for LFA-1 and involves in leukocytes binding to endothelial cells process. It has been reported that abnormal expression of E-selectin and ICAM-1 are correlated with a variety of cancers [2].

A-205804 is a selective E-selectin and ICAM-1 inhibitor over VCAM-1. When tested with primary HUVECs cells, A-205804 treatment reduced cell migration ability by inhibiting the expression of E-selectin and ICAM-1 [3]. In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations [1]. Further, it was revealed that A-205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs) [4].

References:
[1].  Stewart, A.O., et al., Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem, 2001. 44(6): p. 988-1002.
[2].  Chang, C.Z., et al., Valproic acid attenuates intercellular adhesion molecule-1 and E-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. J Inflamm (Lond), 2015. 12: p. 27.
[3].  Zhu, G.D., et al., Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem, 2001. 44(21): p. 3469-87.
[4].   Zhu, G.D., et al., Synthesis and mode of action of (125)I- and (3)H-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. J Org Chem, 2002. 67(3): p. 943-8.