Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Benzocaine 作用电压门控 Na+通道的共同受体,+30 mV 下的 IC50为0.8 mM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
500 mg | ¥ 415 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 466 | 现货 |
产品描述 | Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings. |
靶点活性 | Na+ channel:0.8 mM (IC50) |
体外活性 | Benzocaine blocks μ1 wild-type Na+ currents in a dose-dependent manner with IC50 of 0.8 mM in HEK293T cells. Benzocaine (1 mM) blocks about 55% of wild-type Na+ current but about 95% of μ1-N1584A mutant current. Benzocaine (1 mM) blocks about 55% of wild-type μ1 currents, but about 80% of μ1-I1575A mutant current. [1] Benzocaine results in a biphasic (protective/inductive) concentration-dependent hemolytic effect upon rat erythrocytes, with an effective Benzocaine:lipid molar ratio in the membrane for protection (RePROT), onset of hemolysis (ReSAT) and 100% membrane solubilization (ReSOL) of 1.0:1, 1.1:1 and 1.3:1, respectively. [2] Benzocaine and 4-hydroxybenzoate interact with the open and inactivated channels during repetitive pulses, but during the interpulse the complex dissociates too fast to accumulate sufficient use-dependent block of Na+ currents. [3] Benzocaine (500 μM) reduces the peak and steady-state currents and increases the amplitude of the inactivating component from 21.7% to 30.2% (n=7, P<0.05), so that benzocaine-induced block at the end of pulses to +60 mV averaged 30.9% (n=7). Benzocaine (500 μM) significantly accelerates the initial phase of deactivation (τf=27.2±2.6 ms, n=7, P<0.01), but does not modify the slow phase of tail current decline. Benzocaine binds with high affinity to an intracellular binding site to produce 'agonist' effects and to a low affinity subsite, which is also located in the inner mouth, to produce the blocking effects. Benzocaine and extracellular K(+) interact to modify the voltage-dependence of channel opening. [4] |
体内活性 | Benzocaine is absorbed rapidly and similarly through both viable and nonviable skin of the hairless guinea pig, the absorption of the two acidic compounds, benzoic acid and PABA, is greater through nonviable skin. [5] |
别名 | 苯唑卡因, 苯佐卡因 |
分子量 | 165.19 |
分子式 | C9H11NO2 |
CAS No. | 94-09-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (302.68 mM)
Ethanol: 31 mg/mL (187.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 6.0536 mL | 30.2682 mL | 60.5364 mL | 151.3409 mL |
5 mM | 1.2107 mL | 6.0536 mL | 12.1073 mL | 30.2682 mL | |
10 mM | 0.6054 mL | 3.0268 mL | 6.0536 mL | 15.1341 mL | |
20 mM | 0.3027 mL | 1.5134 mL | 3.0268 mL | 7.567 mL | |
50 mM | 0.1211 mL | 0.6054 mL | 1.2107 mL | 3.0268 mL | |
100 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5134 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Benzocaine 94-09-7 Immunology/Inflammation Membrane transporter/Ion channel Others Sodium Channel MRP Na channels 34584 苯唑卡因 Na+ channels Inhibitor inhibit 苯佐卡因 inhibitor