Clopidogrel hydrogen sulfate 是一种抗血小板药物，可防止血栓形成。Clopidogrel hydrogen sulfate 抑制CYP2B6和CYP2C19，IC,sub>50分别为 18.2 nM 和 524 nM。 Clopidogrel hydrogen sulfate 是一种有效的抗血栓剂，可抑制 ADP 诱导的血小板聚集。Clopidogrel hydrogen sulfate 也是一种具有口服活性 P2Y(12) 抑制剂。
| 生物活性 | Clopidogrel hydrogen sulfate is anantiplateletagent to prevent blood clots. Clopidogrel hydrogen sulfate inhibitsCYP2B6andCYP2C19withIC50s of 18.2 nM and 524 nM, respectively[1]. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation[2]．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor[5]. |
| IC50& Target[1] | CYP2B6 18.2 nM (IC50) | CYP2C19 524 nM (IC50) |
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体外研究
(In Vitro) | Clopidogrel (1.5 mM;12 and 24 hours) up-regulates the expression of TRIB3 and CHOP in a concentration- and time-dependent manner, as measured by real-time PCR and Western blot analysis[3].
Clopidogrel (1.5 mM; 24 hours) significantly induces human gastric epithelial cell (GES-1) apoptosis[3].
Western Blot Analysis[3] | Cell Line: | GES-1 cells | | Concentration: | 1.5 mM | | Incubation Time: | 12 and 24 hours | | Result: | The mRNA expression levels of both CHOP and TRIB3 were up-regulated in a concentration- and time-dependent manner.
The protein expression levels of both CHOP and TRIB3 were up-regulated in a concentration- and time-dependent manner. |
Apoptosis Analysis[3] | Cell Line: | Gastric epithelial cell (GES-1) cells | | Concentration: | 1.5 mM | | Incubation Time: | 24 hours | | Result: | Induced apoptosis of gastric epithelial cells． |
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体内研究
(In Vivo) | Clopidogrel (5 mg/kg) significantly inhibits thrombus formation compared with vehicle. Acetylsalicylic acid (0.15 mg/kg) can add to the antithrombotic effect of Clopidogrel in mice; Acetylsalicylic acid (0.6 mg/kg) blunts the antithrombotic effect of Clopidogrel[4].
| Animal Model: | Age-matched C57BL/6J male mice weighing at least 25 g were used at 8 to 12 weeks of age[4] | | Dosage: | 5 mg/kg | | Administration: | Gavage treatment | | Result: | Clopidogrel significantly inhibited thrombus formation compared with vehicle.
When Clopidogrel was given in combination with 0.6 mg/kg ASA, thrombi were significantly larger than those measured with Clopidogrel alone.
In contrast, when Clopidogrel was given in combination with 0.15 mg/kg ASA , thrombi were significantly smaller than those in mice treated with Clopidogrel and 0.6 mg/kg ASA, and smaller than those in mice given Clopidogrel alone. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 46.7 mg/mL(111.22 mM) H2O : 16.67 mg/mL(39.70 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.3815 mL | 11.9076 mL | 23.8152 mL | | 5 mM | 0.4763 mL | 2.3815 mL | 4.7630 mL | | 10 mM | 0.2382 mL | 1.1908 mL | 2.3815 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 (sealed storage, away from moisture)。-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： PBS Solubility: 50 mg/mL (119.08 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.95 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
