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

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

Bupivacaine HCl 是一种氨基酰胺类局部麻醉剂，可与钠通道胞内结构域结合，阻断钠离子内流，常用于神经传导及心律调控研究。

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Type HazMat fee for 500 gram (Estimated)
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Bupivacaine HCl/盐酸布比卡因 化学结构 CAS号：18010-40-7
Bupivacaine HCl/盐酸布比卡因 化学结构
CAS号：18010-40-7
Bupivacaine HCl/盐酸布比卡因 3D分子结构
CAS号：18010-40-7
Bupivacaine HCl/盐酸布比卡因 化学结构 CAS号：18010-40-7
Bupivacaine HCl/盐酸布比卡因 3D分子结构 CAS号：18010-40-7
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Bupivacaine HCl/盐酸布比卡因 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%
Triamterene +++

ENaC, IC50: 4.5 μM

 		98%
Lamotrigine ✔ 98%
Vinpocetine ✔ 98%
Zonisamide ✔ 99%
Dronedarone HCl ✔ 95%
Procainamide HCl ✔ 99%
Bupivacaine HCl ✔ 99+%
Benzocaine ✔ 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

 		98%
Quinidine sulfate dihydrate ✔ 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%
Amiloride HCl dihydrate ✔ 97%
Ambroxol 98+%
Primidone ✔ 99%
Propafenone ✔ 99%
A-803467 ++++

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

 		99%+
Rufinamide ✔ 99%
Phenytoin sodium ✔ 98%
Proparacaine HCl +

Voltage-gated sodium channel, ED50: 3.4 mM

 		98+%
Amiloride HCl ✔ 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/盐酸布比卡因 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/盐酸布比卡因 细胞实验

Cell Line
Concentration Treated Time Description References
U251MG cells 0.01-0.5 mg/mL 24 hours To evaluate the cytotoxicity of BNC-nanogels, BNCs, empty nanogels, and bupivacaine hydrochloride solution. Results showed that BNC-nanogels at the highest concentration (0.5 mg/mL) reduced cell viability to approximately 59% in U251MG. ACS Appl Mater Interfaces. 2021 Apr 21;13(15):17220-17235.
Mouse mesenchymal stem cells (mMSCs) 0.01-0.5 mg/mL 24 hours To evaluate the cytotoxicity of BNC-nanogels, BNCs, empty nanogels, and bupivacaine hydrochloride solution. Results showed that BNC-nanogels at the highest concentration (0.5 mg/mL) reduced cell viability to approximately 50% in mMSCs. ACS Appl Mater Interfaces. 2021 Apr 21;13(15):17220-17235.
Macrophages 0.01-0.5 mg/mL 24 hours To evaluate the cytotoxicity of BNC-nanogels, BNCs, empty nanogels, and bupivacaine hydrochloride solution. Results showed that macrophages maintained viability similar to the control group (approximately 100%) at all concentrations. ACS Appl Mater Interfaces. 2021 Apr 21;13(15):17220-17235.
Human dermal fibroblasts 0.01-0.5 mg/mL 24 hours To evaluate the cytotoxicity of BNC-nanogels, BNCs, empty nanogels, and bupivacaine hydrochloride solution. Results showed that BNC-nanogels at the highest concentration (0.5 mg/mL) reduced cell viability to approximately 59% and 50% in U251MG and mMSCs, respectively, but maintained viability above 70% in fibroblasts and macrophages. ACS Appl Mater Interfaces. 2021 Apr 21;13(15):17220-17235.
C2C12 mouse myoblasts 0.0025% to 0.125% w/v 2 hours to 3 weeks To evaluate the cytotoxic effects of bupivacaine on C2C12 cells. Results showed that bupivacaine cytotoxicity increased with concentration and exposure duration. For example, 0.025% w/v bupivacaine resulted in 62±12% cell survival after 2h exposure, but only 1±2% after 3 weeks. Anesthesiology. 2008 May;108(5):921-8.
PC12 cells 0.5 mg/mL 7 days To assess the neurotoxicity of bupivacaine on PC12 cells, results showed that neurotoxicity increased with concentration and duration of exposure. Proc Natl Acad Sci U S A. 2009 Apr 28;106(17):7125-30.
C2C12 cells 0.5 mg/mL 4 days To assess the myotoxicity of bupivacaine on C2C12 cells, results showed that myotoxicity increased with concentration and duration of exposure. Proc Natl Acad Sci U S A. 2009 Apr 28;106(17):7125-30.
HEK293 cells 5, 25, 50, 100, 200 μM To test the inhibitory effect of bupivacaine on TASK-1/TASK-3 heterodimeric channels Anesthesiology. 2011 Nov;115(5):1003-11.

Bupivacaine HCl/盐酸布比卡因 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Adult male Sprague-Dawley rats Sciatic nerve blockade model Perisciatic injection 0.5% w/v bupivacaine hydrochloride solution, 10% w/w bupivacaine DAL particles, or 50% w/w bupivacaine PLGA microspheres Single injection To evaluate the myotoxicity of bupivacaine and its sustained-release formulations. Results showed that bupivacaine-loaded microparticles (DAL and PLGA) caused more severe myotoxicity than bupivacaine solution. Anesthesiology. 2008 May;108(5):921-8.
Mice Hip arthroplasty-induced heterotopic ossification model Local injection 10 mg/kg 24 hours before surgery and every 3 days post-surgery for 3 weeks To evaluate the inhibitory effect of bupivacaine lipid nanoparticles on heterotopic ossification, results showed a 50% reduction in bone volume with bupivacaine treatment Bone Res. 2024 Sep 26;12(1):54
Mice TASK-1−/−:TASK-3−/− double knockout mice Intravenous injection 2.5, 3.75, 5, 6.25, 7.5 mg/kg Single or multiple administrations, with at least a week interval between applications To evaluate bupivacaine-induced seizures, TASK knockout mice showed reduced sensitivity to seizure induction Anesthesiology. 2011 Nov;115(5):1003-11.
Male Sprague-Dawley rats Bupivacaine-induced cardiotoxicity model Intravenous injection 10 mg/kg Single dose To evaluate the effect of GPR40 antagonist GW1100 pre-treatment on bupivacaine-induced cardiotoxicity. Results showed that GW1100 pre-treatment prevented lipid emulsion rescue, with no recovery of cardiac function after 10 min. Anesthesiology. 2018 Jul;129(1):154-162
Mice Ovariectomized mouse model Intradermal injection 0.25% and 0.5% Single administration before surgery To assess the effect of bupivacaine on cutaneous wound healing. Results showed that bupivacaine at clinically relevant doses did not impair the rate of wound healing in mice but increased the activity of the degradative enzyme MMP-2. Br J Anaesth. 2010 Jun;104(6):768-73
C57BL/6 mice Repeated social defeat (RSD) model Subcutaneous injection 0.08% Once daily for six days Bupivacaine blocked stress-induced mechanical allodynia but did not affect neuroimmune activation or social avoidance behavior. Brain Behav Immun. 2018 Mar;69:113-123

Bupivacaine HCl/盐酸布比卡因 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/盐酸布比卡因 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/盐酸布比卡因 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/盐酸布比卡因 技术信息

CAS号18010-40-7
分子式C18H29ClN2O
分子量 324.89
SMILES Code O=C(C1N(CCCC)CCCC1)NC2=C(C)C=CC=C2C.[H]Cl
MDL No. MFCD00078956
别名 Bupivacaine (hydrochloride); (±)-1-butyl-2′,6′-Pipecoloxylidide; AH 2250; Bupivacaine hydrochloride
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place,Sealed in dry,2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案 一

Tags: Bupivacaine | 18010-40-7 | iGluR Inhibitor | Neuronal Signaling | Membrane Transporter/Ion Channel | iGluR | Sodium Channel | Calcium Channel | Potassium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Bupivacaine HCl/盐酸布比卡因 纯度/质量文件 | Bupivacaine HCl/盐酸布比卡因 亚型比较 | Bupivacaine HCl/盐酸布比卡因 生物活性 | Bupivacaine HCl/盐酸布比卡因 临床数据 | Bupivacaine HCl/盐酸布比卡因 参考文献 | Bupivacaine HCl/盐酸布比卡因 实验方案 | Bupivacaine HCl/盐酸布比卡因 技术信息

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