Rafigrelide (3,3-Dimethylanagrelide)
(Synonyms: 3,3-Dimethylanagrelide) 目录号 : GC32641
Rafigrelide (3,3-Dimethylanagrelide) 是一种血小板降低剂，也具有抗血栓形成的特性。
Cas No.:1029711-88-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rafigrelide is a platelet-lowering agent, and also has antithrombotic properties.
[1]. Balasubramaniam K, et al. Antithrombotic properties of rafigrelide: a phase 1, open-label, non-randomised, single-sequence, crossover study. Thromb Haemost. 2014 Jul 3;112(1):205-15.
| Cas No. | 1029711-88-3 | SDF | |
| 别名 | 3,3-Dimethylanagrelide | ||
| Canonical SMILES | O=C1NC2=NC3=C(C(Cl)=C(Cl)C=C3)CN2C1(C)C | ||
| 分子式 | C12H11Cl2N3O | 分子量 | 284.14 |
| 溶解度 | DMSO : 1.11 mg/mL (3.91 mM; ultrasonic and warming and heat to 60°C) | 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 | 3.5194 mL | 17.597 mL | 35.1939 mL |
| 5 mM | 0.7039 mL | 3.5194 mL | 7.0388 mL |
| 10 mM | 0.3519 mL | 1.7597 mL | 3.5194 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。
Antithrombotic properties of Rafigrelide: a phase 1, open-label, non-randomised, single-sequence, crossover study
Thromb Haemost 2014 Jul 3;112(1):205-15.PMID:24553755DOI:10.1160/TH13-08-0681
Platelets play a central role in atherothrombotic events. We investigated the effect of a novel platelet-lowering agent, Rafigrelide, on thrombus formation and characteristics. In this phase 1, open-label, non-randomised, single-sequence, crossover study, healthy male volunteers received Rafigrelide for 14 days (Period 1). Following a ≥6-week washout period, they then received Rafigrelide + acetylsalicylic acid (ASA) for 14 days (Period 2). Thrombus formation was assessed ex vivo using the Badimon perfusion chamber, and thrombus characteristics were assessed using thromboelastography. A total of 15 volunteers were enrolled in the study and were assigned to Panel A or Panel B, which had different schedules of assessments. In Panel A, after treatment with Rafigrelide alone (Period 1), mean (± standard deviation) platelet count was reduced from 283 (± 17) × 10⁹/l at Day 1, to 125 (± 47) × 10⁹/l at Day 14 (n=6) and thrombus area reduced under high and low shear conditions. Reductions in thrombus area under high shear conditions correlated with reductions in platelet count (r²=0.11, p=0.022; n=12). Rafigrelide treatment prolonged clot formation time and reduced clot strength. The addition of ASA to Rafigrelide (Period 2) had no additional effect on platelet count or thrombus area under high or low shear conditions. Similar results were seen in Panel B for all parameters. The most common adverse events (≥3 participants per period) were thrombocytopenia and headache. While confirming the platelet-lowering effects of Rafigrelide, this early phase study also indicates that Rafigrelide has antithrombotic properties under both high and low shear conditions.