A 205804;4-(p-Tolylthio)thieno[2,3-c]pyridine-2-carboxamide;A-205804;4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide;4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxaMide;A 205804,4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxaMide;HMS3269O07;UNII-TP7TB1SSZD;TP7TB1SSZD;4-(p-Tolylsulfanyl)thieno[2,3-c]pyridine-2-carboxamide;C15H12N2OS2;4-((4-Methylphenyl)thio)thieno(2,3-C)pyridine-2-carboxamide;Thieno[2,3-c]pyridine-2-carboxamide, 4-[(4-methylphenyl)thio]-;Thieno(2,3-C)pyridine-2-carboxamide, 4-((4-methylphenyl)thio)-;HMS3;4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxamide
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC 50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
性状
Solid
IC50 & Target[1][2]
IC50: 20 nM (E-selectin), 25 nM (ICAM-1)
体外研究(In Vitro)
A-205804 exhibits Cellular Toxicities for HUVEC with an IC50 of 152 μM.A-205804 is an effective inhibitor of cell-cell adhesion in an in vitro flow experiment, demonstrating relevance in a model physiological system. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
A-205804 (5 mg/kg; p.o.) shows a half-life of 1 hour for rat.
A-205804 (10 mg/kg; p.o.; 3 times per week; for 2 weeks) attenuates the E-selectin expression on the endothelial vascular niche cells in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Stewart AO, 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 Mar 15;44(6):988-1002.[2]. Morita K, et al. RUNX transcription factors potentially control E-selectin expression in the bone marrow vascular niche in mice. Blood Adv. 2018 Mar 13;2(5):509-515.
溶解度数据
In Vitro: DMSO : 100 mg/mL (332.89 mM; ultrasonic and warming and heat to 60°C)配制储备液