YM-254890
目录号 : GC46239A cyclic depsipeptide Gαq/11 inhibitor
Cas No.:568580-02-9
Sample solution is provided at 25 µL, 10mM.
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).
| Cas No. | 568580-02-9 | SDF | |
| 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 SMILES | O=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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0416 mL | 5.2078 mL | 10.4156 mL |
| 5 mM | 0.2083 mL | 1.0416 mL | 2.0831 mL |
| 10 mM | 0.1042 mL | 0.5208 mL | 1.0416 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet