Benzocaine (Synonyms:苯佐卡因)
目录号 : KM20064 CAS No. : 94-09-7 纯度 : 98%

Benzocaine 作用电压门控Na+通道的共同受体,其在 +30 mV 下测得的 IC50 值为0.8 mM。

规格 价格 是否有货 数量
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

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生物活性

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na channel, with an IC50 of 0.8 mM tested with a potential of +30 mV.

体外研究

Benzocaine blocks μ1 wild-type Na currents in a dose-dependent Manner. The Benzocaine concentration that inhibits 50% of Na currents (IC50) is estimated to be about 0.8 mM when a test potential of +30 mV is applied. The slope of the h∞ curve is also significantly reduced by benzocaine (from 6.6 to 9.9 mV). Mutation of μ1-N1584A also significantly increases the potency of Benzocaine. At 1 mM, Benzocaine blocks about 55% of wild-type Na current but about 95% of μ1-N1584A mutant current. Benzocaine also appears to bind more strongly to its LA receptor in the N1584A mutant than in the wild type. The inhibition of Ca uptake occurres at lower Benzocaine concentration (IC50=40.3±1.2mM) than that affecting the enzymatic activity.

体内研究

Benzocaine is topically applied to the following species: dogs, domestic shorthair cats, Long-Evans rats, Sprague-Dawley rats, ferrets, rhesus monkeys, cynomolgus monkeys, owl monkeys, New Zealand White rabbits, miniature pigs, ICR mice, C3H mice, and C57BL/10SnJ mice. All animals, except mice and rats, receive a 2-second spray to the mucous membranes of the nasopharynx for an estimated dose of 56 mg. A 2-second spray to rodents' oral mucous membranes delivers too great a volume of fluid for these animals. The study is repeated in dogs several months later to confirm low response. Response to Benzocaine spray is observed in most animals tested, with response peaking between 15 and 30 minutes after dosing.

分子式
C9H11NO2
分子量
165.19
CAS号
94-09-7
中文名称
苯佐卡因;苯唑卡因;4-氨基苯甲酸乙酯;对氨基苯甲酸乙酯;乙基-4-氨基苯甲酸酯;
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (605.36 mM)

H2O : 2 mg/mL (12.11 mM; ultrasonic and warming and heat to 60°C)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.0536 mL 30.2682 mL 60.5364 mL
5 mM 1.2107 mL 6.0536 mL 12.1073 mL
10 mM 0.6054 mL 3.0268 mL 6.0536 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (15.13 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (15.13 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (15.13 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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科研文献
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