Ticagrelor-d7
(Synonyms: 替卡格雷 d7) 目录号 : GC48180
An internal standard for the quantification of ticagrelor
Cas No.:1265911-55-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ticagrelor-d7 is intended for use as an internal standard for the quantification of ticagrelor by GC- or LC-MS. Ticagrelor is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 14 nM; IC50 = 1.8 μM), which is the main receptor responsible for ADP-induced platelet aggregation.1,2 It functions by directly changing the conformation of the P2Y12 receptor to inhibit ADP binding.3 Formulations containing ticagrelor have been used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome.
1.Zech, G., Hessler, G., Evers, A., et al.Identification of high-affinity P2Y12 antagonists based on a phenylpyrazole glutamic acid piperazine backboneJ. Med. Chem.55(20)8615-8629(2012) 2.Michelson, A.D.Advances in antiplatelet therapyHematology Am. Soc. Hematol. Educ. Program2011(1)62-69(2011) 3.Wallentin, L.P2Y12 inhibitors: Differences in properties and mechanisms of action and potential consequences for clinical useEur. Heart J.30(16)1964-1977(2009)
| Cas No. | 1265911-55-4 | SDF | |
| 别名 | 替卡格雷 d7 | ||
| Canonical SMILES | FC(C(F)=C1)=CC=C1[C@@H]2C[C@H]2NC3=C4C(N([C@@H]5C[C@H](OCCO)[C@@H](O)[C@H]5O)N=N4)=NC(SC([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])=N3 | ||
| 分子式 | C23H21D7F2N6O4S | 分子量 | 529.6 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 15 mg/ml | 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 | 1.8882 mL | 9.4411 mL | 18.8822 mL |
| 5 mM | 0.3776 mL | 1.8882 mL | 3.7764 mL |
| 10 mM | 0.1888 mL | 0.9441 mL | 1.8882 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。
Development and Validation of Simple LC-MS-MS Assay for the Quantitative Determination of Ticagrelor in Human Plasma: its Application to a Bioequivalence Study
J Chromatogr Sci 2019 Apr 1;57(4):331-338.PMID:30715279DOI:10.1093/chromsci/bmz001
A sensitive, rapid, reproducible and reliable high-performance liquid chromatography-electrospray ionization tandem mass spectrometric method has been developed and fully validated for the determination of ticagrelor in human plasma using Ticagrelor-d7 as an internal standard (IS) after one-step liquid-liquid extraction with ethyl acetate. Ticagrelor and IS were detected in the multiple reaction monitoring mode at m/z transition 523.4 > 127.0 and 530.4 > 127.0, respectively. Chromatographic separation was performed on a Phenomenex Luna® C18 column using a mobile phase consisting of 0.1% formic acid in water-acetonitrile (20:80, v/v) at a flow rate of 0.2 mL/min. The retention times of ticagrelor and IS were 1.03 min and 1.02 min, respectively. The calibration curve was linear [correlation coefficient (r) ≥ 0.9991] over the concentration range of 2-1,500 ng/mL. Intra- and inter-day precisions ranged from 1.0% to 4.9% and from 1.8% to 8.7%, and the accuracy ranged from 97.0% to 105.9% and from 97.5% to 102.9%, respectively. The developed method was fully validated with respect to selectivity, linearity, lower limit of quantitation, recovery, matrix effect and stability. This validated method was successfully applied to the bioequivalence study of ticagrelor in 44 healthy Korean male volunteers.