| CAS NO: | 251992-66-2 |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 300.39 |
| Cas No. | 251992-66-2 |
| Formula | C15H12N2OS2 |
| Solubility | ≥30 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide |
| Canonical SMILES | CC1=CC=C(C=C1)SC2=C3C=C(SC3=CN=C2)C(=O)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
A 205804是E-选择素和ICAM-1的高效选择性抑制剂,IC50值分别为20 nM和25 nM[1].
E选择素是一种细胞粘附分子,在炎症过程中募集白细胞至损伤部位中发挥重要作用.ICAM-1(胞内粘附分子1)是LFA-1的配体,参与白细胞结合内皮细胞的过程.有报道称E-选择素和ICAM-1的异常表达与多种癌症相关[2].
A205804是E-选择素和ICAM-1而非VCAM-1的选择性抑制剂.在原代脐静脉内皮细胞(HUVECs)中,A205804处理通过抑制E-选择素和ICAM-1的表达而减少细胞迁移[3].在使用全细胞高通量试验的人血管内皮细胞中,低浓度A205804能够高效选择性抑制E-选择素和ICAM-1[1].而且,人脐静脉内皮细胞(HUVECs)的实验表明A205804通过易位到细胞核,非共价结合分子量超过650KDa的大分子,从而抑制E-选择素和ICAM-1表达[4].
参考文献：
[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.
| Description | A 205804是E-选择素和ICAM-1表达的高效选择性抑制剂,IC50值分别为20 nM和25 nM. | |||||
| 靶点 | E-selectin | ICAM-1 | ||||
| IC50 | 20 nM | 25 nM | ||||
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