| 中文名称: | Ticagrelor 促销 | ||||
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| 英文名称: | Ticagrelor | ||||
| 别名: | 替格瑞洛 AZD6140;(1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino]-5-(propylthio)- 3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol | ||||
| CAS No: | 274693-27-5 | 分子式: | C23H28F2N6O4S | 分子量: | 522.57 |
| CAS No: | 274693-27-5 | ||||
| 分子式: | C23H28F2N6O4S | ||||
| 分子量: | 522.57 | ||||
基本信息
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产品编号： |
T10378 |
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产品名称： |
Ticagrelor |
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CAS: |
274693-27-5 |
储存条件 |
粉末 |
-20℃ |
四年
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分子式： |
溶于液体 |
-80℃(避光，储存于氮) |
6个月 |
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分子量 |
522.57 |
-20℃(避光，储存于氮) |
1个月 |
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化学名： |
(1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino]-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol |
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Solubility (25°C)： |
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体外:
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DMSO |
100mg/mL (191.36mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
2% DMSO+30% PEG 300+5% Tween 80+ddH2O |
10mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.9136mL |
9.5681mL |
19.1362mL |
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5mM |
0.3827mL |
1.9136mL |
3.8272mL |
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10mM |
0.1914mL |
0.9568mL |
1.9136mL |
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50mM |
0.0383mL |
0.1914mL |
0.3827mL |
生物活性
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产品描述 |
一种P2Y12受体的拮抗剂，对血小板聚集有作用。 |
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靶点 |
P2Y12 |
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2nM(Ki) |
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体外研究 |
Ticagrelor promotes a greater inhibition of adenosine 5′-diphosphate (ADP)–induced Ca2+release in ished platelets vs other P2Y12R antagonists. This additional effect of ticagrelor beyond P2Y12R antagonism is in part as a consequence of ticagrelor inhibiting the equilibrative nucleoside transporter 1 (ENT1) on platelets, leading to accumulation of extracellular adenosine and activation of Gs-coupled adenosine A2A receptors.B16-F10 cells exhibit decreased interaction with platelets from ticagrelor-treated mice compared to saline-treated mice. |
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体内研究 |
In B16-F10 melanoma intravenous and intrasplenic metastasis models,mice treated with a clinical dose of ticagrelor (10mg/kg) exhibits marked reductions in lung (84%) and liver (86%) metastases.Furthermore,ticagrelor treatment improves survival compared to saline-treated animals.A similar effect is observed in a 4T1 breast cancer model,with reductions in lung (55%) and bone marrow (87%) metastases following ticagrelor treatment.Single oral administration of ticagrelor (1-10mg/kg) causes dose-related inhibitory effect on platelet aggregation.Ticagrelor,at the highest dose (10mg/kg) significantly inhibits platelet aggregation at 1h after dosing and the peak inhibition is observed at 4h after dosing. |
推荐实验方法(仅供参考)
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激酶实验： |
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使用P2Y12转染的 CHO-K1或人血小板细胞膜进行的结合试验 |
将膜(5微克蛋白质)加入96孔板，孔板中含有[125I]AZ11931285 (125pM)，[3H]ADP (10nM)，或[33P]2MeS-ADP (62.5pM)，需要的竞争剂浓度，以及充足体积的缓冲液(50mM Tris，5mM MgCl2，50mM NaCl，和0.1% 不含核苷酸的BSA，pH 7.4)，使每孔总体积为200微升。结合研究使用血小板膜和[3H]ADP在100μM (终浓度) MRS2179存在下进行，以阻止与P2Y1的结合。P2Y12转染的CHO-K1细胞的信噪比，对[3H]ADP (特征信号: 895 c.p.m.)大约为14，对[33P]2MeSADP (特征信号: 3308 c.p.m.)大约为24，对[125I]AZ11931285 (特征信号: 3308 c.p.m.)大约为24。对于使用血小板膜的研究中，[33P]2MeS-ADP和[3H]ADP的信噪比大约为2，[125I]AZ11931285的为1.5，特定信号为100到400 c.p.m。在该研究中，在30℃下培育1小时可以达到完全平衡。随后，游离放射性配体从结合配体中分离，并如上进行计数。 |
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动物实验: |
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Rats:Prasugrel (10mg/kg,p.o.) and ticagrelor (30mg/kg,p.o.),doses that produced similar levels of inhibition of platelet aggregation,are administered to rats 4h before the bleeding time measurements. Fresh, washed platelets (1×1010 platelets/mL) are prepared from other rats and suspended in Hank's balanced salt solution.Platelets are transfused via the jugular vein to rats 1h before the bleeding time measurements and the bleeding time is determined. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
