Bupivacaine hydrochloride 是一种NMDA受体抑制剂。Bupivacaine 可以阻断钠、L-钙和钾通道。Bupivacaine 有效阻断SCN5A通道，IC50为 69.5 μM。Bupivacaine hydrochloride 可用于慢性疼痛的研究。
| 生物活性 | Bupivacaine hydrochloride is aNMDA receptorinhibitor.Bupivacaine can blocksodium,L-calcium, andpotassium channels.Bupivacaine potently blocksSCN5A channelswith theIC50of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain[1][2][3]. |
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体外研究
(In Vitro) | Bupivacaine hydrochloride inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization[1].
Bupivacaine hydrochloride influences the voltage dependency of channel activation and steady-state inactivation by shifting the membrane potential of half-maximal activation/inactivation toward somewhat more negative membrane potentials. In their inactivated state, SCN5A channels are slightly sensitive toward Bupivacaine hydrochloride IC50=2.18±0.16 μM[2].
Bupivacaine hydrochloride reversibly inhibits the SK2 channel in a dose-dependent manner with the IC50of 16.5 μM[3].
Cell Viability Assay[3] | Cell Line: | HEK 293 cells transfected with the SK2 gene (transfected cells were named SK2 cells) | | Concentration: | 10, 100, 1000 μM | | Incubation Time: | | | Result: | The IC50value was 16.5 μM. |
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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 and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(76.95 mM;Need ultrasonic) H2O : 12.5 mg/mL(38.47 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.0780 mL | 15.3898 mL | 30.7796 mL | | 5 mM | 0.6156 mL | 3.0780 mL | 6.1559 mL | | 10 mM | 0.3078 mL | 1.5390 mL | 3.0780 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 and light)。-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: 13 mg/mL (40.01 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.69 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.69 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 25.0 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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