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Levobupivacaine hydrochloride

Levobupivacaine hydrochloride

产品编号 T6566   CAS 27262-48-2
别名: Levobupivacaine HCl, (S)-(-)-Bupivacaine HCl, 盐酸左布比卡因, (S)-(-)-Bupivacaine monohydrochloride

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是有效的钠通道阻滞剂。

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Levobupivacaine hydrochloride Chemical Structure
Levobupivacaine hydrochloride, CAS 27262-48-2
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
其他形式的 Levobupivacaine hydrochloride:
千万补贴 助力科研
产品目录号及名称: Levobupivacaine hydrochloride (T6566)
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纯度: 99.93%
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生物活性
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 53 mg/mL (163.1 mM)

H2O: 59 mg/mL (181.6 mM)

DMSO: 60 mg/mL (184.7 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Foster RH, et al. Drugs, 2000, 59(3), 551-579. 2. Vladimirov M, et al. Anesthesiology, 2000, 93(3), 744-755. 3. Kanai Y, et al. Anesth Analg, 2000, 90(2), 415-420. 4. Gristwood RW, et al. Expert Opin Investig Drugs, 1999, 8(6), 861-876.
Piromelatine Quinidine hydrochloride monohydrate Eleclazine hydrochloride L-Aspartic aicd sodium EIPA A-803467 3-Deoxyaconitine Ralfinamide

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 药物功能重定位化合物库 抗癌上市药物库 膜蛋白靶向化合物库 抗癌临床化合物库 抗癌药物库 临床期小分子药物库 FDA上市及药典收录分子库 经典已知活性库 抗心血管疾病化合物库

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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。

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Keywords

Levobupivacaine hydrochloride 27262-48-2 Membrane transporter/Ion channel Sodium Channel CNS toxicity gastric cancer Na channels Erastin Inhibitor analgesic anaesthetic Levobupivacaine Hydrochloride Na+ channels cardiac toxicity Bupivacaine HCl CYP450 Levobupivacaine HCl Ferroptosis (S)-(-)-Bupivacaine HCl 盐酸左布比卡因 inhibit (S)-(-)-Bupivacaine monohydrochloride Levobupivacaine NMDA Bupivacaine Bupivacaine Monohydrochloride inhibitor

 

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