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YM-254890
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
YM-254890图片
CAS NO:568580-02-9
包装:1mg
市场价:4914元

YM-254890 是一种从 Chromobacterium sp. 中分离出来的选择性 Gαq/11 蛋白抑制剂。
Cas No.568580-02-9
化学名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-L-threonine(7→1)-lactone
Canonical SMILESO=C(N[C@@H](C)C1=O)C(N(C)C([C@H](OC([C@@H](NC(C)=O)[C@H](OC([C@@]([C@@H](C)OC)([H])N(C)C([C@@]([C@@H](C(C)C)OC([C@H]([C@H](O)C(C)C)NC(C)=O)=O)([H])NC([C@@H](N1C)C)=O)=O)=O)C)=O)CC2=CC=CC=C2)=O)=C
分子式C46H69N7O15
分子量960.1
溶解度10mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

YM-254890 is cyclic depsipeptide originally isolated from Chromobacterium and an inhibitor of Gαq/11.[1] It inhibits Gαq/11-mediated intracellular calcium mobilization induced by 2MeSADP or methacholine in C6-15 cells expressing the purinergic P2Y1 receptor (IC50 = 0.15 μM) and in CHO cells expressing M1 muscarinic acetylcholine receptors (IC50 = 0.15 μM), respectively, but has no effect on Gαi-mediated calcium mobilization induced by fMLP in HL-60 cells (IC50 = >10 μM). YM-254890 inhibits platelet aggregation induced by ADP, collagen, thrombin receptor agonist peptide (TRAP), arachidonic acid , or U-46619 in isolated human platelet-rich plasma (IC50s = 0.39, 0.15, 0.71, 0.25, and 0.34 μM, respectively).[2] It reduces shear stress-induced thrombus formation in isolated human whole blood. YM-254890 (1, 3, and 10 μg/kg) reduces platelet thrombus formation in a cynomolgus monkey model of femoral artery thrombosis.

Reference:
[1]. Takasaki, J., Saito, T., Taniguchi, M., et al. A Novel Gɑq/11-selective Inhibitor. J. Biol. Chem. 279(46), 47438-47445 (2004).
[2]. Uemura, T., Kawasaki, T., Taniguchi, M., et al. Biological properties of a specific Gɑq/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress. Br. J. Pharmacol. 148(1), 61-69 (2006).

 
 
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