| CAS NO: | 568580-02-9 |
| 生物活性 | YM-254890 is a selectiveGαq/11proteininhibitor isolated fromChromobacteriumsp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking theP2Y1signal transduction pathway, with anIC50value below 0.6 μM[1][2]. | |||||||||
| IC50& Target | Gαq/11protein[1][2] | |||||||||
| 体外研究 (In Vitro) | YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC50values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y1and P2Y12. The effect of YM-254890 on the P2Y1and P2Y12signal transduction pathways using C6-15 cells stably expressing the human P2Y1or P2Y12receptors is examined. Stimulation of P2Y1-C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca2+]iwith an IC50value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y12-C6-15 cells is unaffected by YM-254890 at 40 μM[1]. | |||||||||
| 分子量 | 960.08 | |||||||||
| 性状 | Solid | |||||||||
| Formula | C46H69N7O15 | |||||||||
| CAS 号 | 568580-02-9 | |||||||||
| 结构分类 |
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| 来源 | the culture broth of Chromobacterium sp | |||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||
| 储存方式 |
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