Bupivacaine

产品编号 T0030LCas号 38396-39-3

别名 布比卡因|||AH 250|||AH-250|||AH250|||Bupivacaina|||Exparel|||Anekain

Bupivacaine (AH-250) 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 可用于慢性疼痛的研究。

产品编号 T0030L别名 布比卡因, AH 250, AH-250, AH250, Bupivacaina, Exparel, AnekainCas号 38396-39-3

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生物活性

产品描述	Bupivacaine (AH-250) is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine can be used for the research of chronic pain.
体外活性	Bupivacaine inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization[1]. Bupivacaine 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 IC50=2.18±0.16 μM[2]. Bupivacaine reversibly inhibits the SK2 channel in a dose-dependent manner with the IC 50 of 16.5 µM[3].
别名	布比卡因, AH 250, AH-250, AH250, Bupivacaina, Exparel, Anekain

化学信息

储存&溶解度

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 25 mg/mL (86.69 mM)

溶液配制表

DMSO