Vinpocetine (Ethyl apovincaminate) 是一种长春花生物碱衍生物,可阻断 Na+通道。Vinpocetine 抑制IKK的IC50值为 17.17 μM。Vinpocetine 还是PDE抑制剂,并通过直接靶向IKK抑制NF-κB依赖性炎症反应,已被广泛用于研究脑血管疾病。
生物活性 | Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+channels. TheIC50value of Vinpocetine on directIKKinhibition in the cell-free system is 17.17 μM. Vinpocetine is aphosphodiesterase (PDE)inhibitor and inhibitsNF-κB-dependent inflammatory responses by directly targetingIκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders[1][2][3]. |
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体外研究 (In Vitro) | Vinpocetine (5-50 μM; 7 hours; VSMCs, HUVECs, A549 cells and RAW264.7 cells) potently inhibits TNF-α-induced NF-κB-dependent transcriptional activity in a dose-dependent manner with an approximateIC50value of 25 μM. Vinpocetine do not have a significant effect on cell viability[1]. Vinpocetine (50 μM; 7 hours; VSMCs, HUVECs, A549 cells and RAW264.7 cells) potently inhibits TNF-α-induced up-regulation of TNF-α, IL-1β, IL-8, MCP-1, VCAM-1, ICAM-1and MIP-2 transcripts in several cell types[1].
RT-PCR[1] Cell Line: | VSMCs, HUVECs, A549 cells and RAW264.7 cells | Concentration: | 50 μM | Incubation Time: | 7 hours | Result: | Inhibited TNF-α-induced up-regulation of TNF-α, IL-1β, IL-8, MCP-1, VCAM-1, ICAM-1and MIP-2 transcripts in several cell types. |
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体内研究 (In Vivo) | Vinpocetine (2.5-10 mg/kg; intraperitoneal injection; C57BL/6 mice) potently inhibits TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreases interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation[1].
Animal Model: | C57BL/6 mice (8 weeks of age)[1] | Dosage: | 2.5 mg/kg, 5 mg/kg, and 10 mg/kg | Administration: | Intraperitoneal injection | Result: | Inhibited TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreased interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation. |
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中文名称 | 长春西汀;长春西丁;长春乙酯;卡兰;阿扑长春胺酸乙酯;长春酸乙酯 |
结构分类 | - Alkaloids
- Piperidine Alkaloids
- Alkaloids
- Indole Alkaloids
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来源 | - Plants
- Apocynaceae
- Catharanthus roseus(L.) G. Don
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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: Ethanol : 7.14 mg/mL(20.37 mM;Need ultrasonic) DMSO : 6.25 mg/mL(17.83 mM;Need ultrasonic) 配制储备液 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL | 5 mM | 0.5707 mL | 2.8535 mL | 5.7069 mL | 10 mM | 0.2853 mL | 1.4267 mL | 2.8535 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: ≥ 0.62 mg/mL (1.77 mM); Clear solution
此方案可获得 ≥ 0.62 mg/mL (1.77 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 6.2 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 0.62 mg/mL (1.77 mM); Clear solution
此方案可获得 ≥ 0.62 mg/mL (1.77 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 6.2 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: ≥ 0.62 mg/mL (1.77 mM); Clear solution
此方案可获得 ≥ 0.62 mg/mL (1.77 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 6.2 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。
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