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盐酸布比卡因 /Bupivacaine HCl {[allProObj[0].p_purity_real_show]}

货号:A540958 同义名: Bupivacaine (hydrochloride);(±)-1-butyl-2′,6′-Pipecoloxylidide

Bupivacaine HCl is a local anaesthetic drug belonging to the amino amide group.

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Bupivacaine HCl 化学结构 CAS号:18010-40-7
Bupivacaine HCl 化学结构
CAS号:18010-40-7
Bupivacaine HCl 3D分子结构
CAS号:18010-40-7
Bupivacaine HCl 化学结构 CAS号:18010-40-7
Bupivacaine HCl 3D分子结构 CAS号:18010-40-7
规格 价格 会员价 库存 数量
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Bupivacaine HCl 纯度/质量文件 产品仅供科研

货号:A540958 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl 99%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 98%
Dronedarone Hydrochloride 95%
Procainamide hydrochloride 99%
Bupivacaine HCl 99+%
Benzocaine 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

98%
Ibutilide fumarate 99%+
Dibucaine HCl 99+%
Mexiletine HCl 99%
Phenytoin 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

99%+
Levobupivacaine 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

98%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

99%+
Rufinamide 99%
Phenytoin sodium 98%
Proparacaine Hydrochloride +

Voltage-gated sodium channel, ED50: 3.4 mM

98+%
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Bupivacaine HCl 生物活性

靶点
  • Sodium Channel

描述 Bupivacaine has a strong affinity for SCN5A channels with an IC50 of 69.5 µM, making it valuable for chronic pain research[1].[2].[3].
体外研究

Additionally, Bupivacaine hydrochloride disrupts NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, a key region involved in central sensitization, a mechanism underlying the development of persistent pain[1].

The drug also modifies the voltage dependency of channel activation and steady-state inactivation. It shifts the membrane potential required for half-maximal activation/inactivation toward more negative potentials, which affects the channels' sensitivity to the drug. Specifically, in their inactivated state, SCN5A channels exhibit some sensitivity to Bupivacaine hydrochloride with an IC50 of approximately 2.18 ± 0.16 μM[2].

Moreover, Bupivacaine hydrochloride can reversibly inhibit the SK2 channel in a dose-dependent manner, demonstrating an IC50 of 16.5 µM[3].

Bupivacaine HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02679560 Femoral Fractures Phase 2 Recruiting April 2019 United States, California ... 展开 >> University of California Davis Med Center- Emergency Department Recruiting Sacramento, California, United States, 95817 Contact: Ian Brown, MD    916-734-1279    iebrown@ucdavis.edu 收起 <<
NCT02287623 Acute Pain Phase 4 Completed - -
NCT01429584 - Completed - -

Bupivacaine HCl 参考文献

[1]Casati A, et, al. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different? Best Pract Res Clin Anaesthesiol. 2005 Jun;19(2):247-68.

[2]Dan J, et, al. Inhibition of gastric cancer by local anesthetic bupivacaine through multiple mechanisms independent of sodium channel blockade. Biomed Pharmacother. 2018 Jul;103:823-828.

[3]Carsten Stoetzer, et al. Inhibition of Voltage-Gated Na+ Channels by Bupivacaine Is Enhanced by the Adjuvants Buprenorphine, Ketamine, and Clonidine. Reg Anesth Pain Med.Jul/Aug 2017;42(4):462-468.

Bupivacaine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.39mL

3.08mL

1.54mL

30.78mL

6.16mL

3.08mL

Bupivacaine HCl 技术信息

CAS号18010-40-7
分子式C18H29ClN2O
分子量 324.889
别名 Bupivacaine (hydrochloride);(±)-1-butyl-2′,6′-Pipecoloxylidide;AH 2250;Bupivacaine hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度
动物实验配方
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