Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是有效的钠通道阻滞剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 278 | 现货 | ||
25 mg | ¥ 452 | 现货 | ||
50 mg | ¥ 578 | 现货 | ||
100 mg | ¥ 767 | 现货 | ||
200 mg | ¥ 995 | 现货 | ||
500 mg | ¥ 1,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 242 | 现货 |
产品描述 | Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor, which is the pure S(-)-enantiomer of bupivacaine. It was utilized as a long-acting local anesthetic. |
体外活性 | Levobupivacaine is an amide-type local anaesthetic. Levobupivacaine acts via blockade of voltage-sensitive ion channels in neuronal membranes, preventing transmission of nerve impulses. Localised and reversible anaesthesia is produced by interference with the opening of the sodium channel, which inhibits conduction of the action potential in nerves involved in sensory and motor activity and sympathetic activity. [1] Levobupivacaine displaces 3H-BTX from sodium channels of rat brain synaptosomes with IC50 of 2.9 μM and Hill coefficients of 1.2. When cell membrane is held at -80 mV, -70 mV, -60 mV or -100 mV, Levobupivacaine shows tonic inhibition of sodium channel in GH3 cells with IC50s of 132.1, 37.6, 21.6 and 264 μM, respectively. [2] Levobupivacaine depresses action potential of isolated axon in vitro. Levobupivacaine (1 mM) depresses action potential amplitude and maximal rate of rise of action potential (dV/dtmax) in the crayfish giant axons with value of 88 and 81 respectively, after perfusion for 15 min. [3] Levobupivacaine also displays activity on cardiac ion channels. In isolated ventricular myocytes, the apparent affinity for inactivated state of the sodium channel is 4.8 μM for Levobupivacaine, with a calculated KD of 39 μM. On inhibition of cardiac delayed rectifier potassium channels (hKv1.5), the steady-state block for Levobupivacaine (20 μM) is 31%, with a calculated KD of 27.3 μM. Levobupivacaine may also inhibit cardiac calcium channels. 10 μM Levobupivacaine produces a 50% decrease in contractile force of guinea-pig papillary muscles. [4] |
体内活性 | Levobupivacaine has similar nerve blocking potency with bupivacaine. Levobupivacaine at a dose of 0.125%, inhibits motor and nocifensive pinch responses with maximum %MPE of 99 and 68 respectively, and inhibits the duration of deficits of motor and nocifensive pinch responses (60 and 30 , respectively) after sciatic nerve block. [4] |
激酶实验 | Hsp90 Binding Assay: Human Hsp90α solution (0.5 μg/mL) is fixed on 96-well plates, followed by blocking with TBS containing 1% bovine serum albumin. KW-2478 solutions is added to the wells, and bRD is added to a concentration of 0.1 μmol/L. After removal of solution, poly-HRP streptavidin solution dilutes with poly-HRP dilution buffer is added to the wells. After removal of solution, equal volumes of TMB peroxidase substrate and peroxidase solution B are added to the wells. To stop the HRP reaction, 2 mol/L H2SO4 are added, followed by measurement of absorbance at 450 nm using a microplate spectrophotometer. |
别名 | Levobupivacaine HCl, (S)-(-)-Bupivacaine HCl, 盐酸左布比卡因, (S)-(-)-Bupivacaine monohydrochloride |
分子量 | 324.89 |
分子式 | C18H28N2O·HCl |
CAS No. | 27262-48-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 53 mg/mL (163.1 mM)
H2O: 59 mg/mL (181.6 mM)
DMSO: 60 mg/mL (184.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / H2O / DMSO | 1 mM | 3.078 mL | 15.3898 mL | 30.7796 mL | 76.9491 mL |
5 mM | 0.6156 mL | 3.078 mL | 6.1559 mL | 15.3898 mL | |
10 mM | 0.3078 mL | 1.539 mL | 3.078 mL | 7.6949 mL | |
20 mM | 0.1539 mL | 0.7695 mL | 1.539 mL | 3.8475 mL | |
50 mM | 0.0616 mL | 0.3078 mL | 0.6156 mL | 1.539 mL | |
100 mM | 0.0308 mL | 0.1539 mL | 0.3078 mL | 0.7695 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。
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