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568580-02-9

中文名稱 L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
英文名稱 L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
CAS 568580-02-9
分子式 C46H69N7O15
分子量 960.08
MOL 文件 568580-02-9.mol
568580-02-9 結(jié)構(gòu)式 568580-02-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 T17273
英文別名
L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone

物理化學性質(zhì)

沸點1232.4±65.0 °C(Predicted)
密度1.26±0.1 g/cm3(Predicted)
儲存條件-20°C
溶解度溶于DMSO(高達10mg/ml)
酸度系數(shù)(pKa)12.52±0.70(Predicted)
形態(tài)凍干固體
顏色白色或灰白色
穩(wěn)定性可在-20°C下的DMSO溶液保存長達1個月。

常見問題列表

生物活性
YM-254890 是一種從 Chromobacterium sp 中分離的選擇性 Gαq/11 蛋白抑制劑。YM-254890 對其他 G 蛋白亞型無抑制作用。YM-254890 通過阻斷 P2Y1 信號轉(zhuǎn)導途徑來抑制 ADP 誘導的血小板凝集,其 IC50 值低于 0.6 μM。
靶點

G αq/11 protein

體外研究

YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC 50 values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y 1 and P2Y 12 . The effect of YM-254890 on the P2Y 1 and P2Y 12 signal transduction pathways using C6-15 cells stably expressing the human P2Y 1 or P2Y 12 receptors is examined. Stimulation of P2Y 1 -C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca 2+ ] i with an IC 50 value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y 12 -C6-15 cells is unaffected by YM-254890 at 40 μM.

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