568580-02-9

中文名称 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

英文名称 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 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T17273

英文别名

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

物理化学性质

沸点1232.4±65.0 °C(Predicted)

密度1.26±0.1 g/cm3(Predicted)

储存条件-20°C

溶解度溶于DMSO（高达10mg/ml）

酸度系数(pKa)12.52±0.70(Predicted)

形态冻干固体

颜色白色或灰白色

稳定性可在-20°C下的DMSO溶液保存长达1个月。

常见问题列表

生物活性

YM-254890 是一种从 Chromobacterium sp 中分离的选择性 Gαq/11 蛋白抑制剂。YM-254890 对其他 G 蛋白亚型无抑制作用。YM-254890 通过阻断 P2Y1 信号转导途径来抑制 ADP 诱导的血小板凝集，其 IC50 值低于 0.6 μM。

靶点

G _αq/11 protein

体外研究

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.