Vicagrel 是一种有效且安全的抗血小板剂，具有口服活性，通过不可逆地抑制 P2Y12 受体起作用。Viagrel 可用于冠状动脉疾病、外周血管疾病和脑血管疾病中血栓的研究。
| 生物活性 | Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibitingP2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease[1][2]. |
体外研究
(In Vitro) | Vicagrel (compound 9a) (20 μM, 30 min) activates production of the active metabolite from in vitro rat liver microsomal[1].
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体内研究
(In Vivo) | Vicagrel (compound 9a) (oral, 3 mg/kg) has inhibitory effect on ADP-induced platelet aggregation in rats[1].
Vicagrel (oral, 1.14 mg/mL, 0-24 h) has giood preliminary pharmacokinetic with high bioavailability and low clinically effective dose[1].
Vicagrel (oral, 5 g/kg, single, for 14 days) has low dose-related toxicity in mouse[1].
| Animal Model: | Male Wistar rats[1]
(200–250 g) | | Dosage: | 3 mg/kg | | Administration: | oral | | Result: | Inhibitied platelet aggregation by ADP-induced in rats. |
| Animal Model: | SD male rats[1] | | Dosage: | 1.14 mg/mL | | Administration: | oral, 0-24 h | | Result: | Could be readily converted into clopidogrel thiolactone and had high bioavailability. |
| Animal Model: | Mice[1] | | Dosage: | 5 g/kg | | Administration: | oral, single, for 14 days | | Result: | Had very low acute toxicity. |
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| Clinical Trial | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(658.14 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6325 mL | 13.1627 mL | 26.3255 mL | | 5 mM | 0.5265 mL | 2.6325 mL | 5.2651 mL | | 10 mM | 0.2633 mL | 1.3163 mL | 2.6325 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.48 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.48 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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