Proparacaine Hydrochloride (Synonyms:盐酸丙美卡因; Proxymetacaine Hydrochloride)
目录号 : KM16883 CAS No. : 5875-06-9 纯度 : 98%

Proparacaine Hydrochloride (Proxymetacaine Hydrochloride) 是 Lidocaine 的衍生物,具有免疫调节作用和糖皮质激素样活性。

规格 价格 是否有货 数量
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Proparacaine Hydrochloride (Proxymetacaine Hydrochloride) is a derivative of lidocaine , with immunomodulatory effect and glucocorticomimetic activity.

体外研究

Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro.
Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells .
Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells.
Proparacaine Hydrochloride induces caspase-2, -3 and -9 activation, and mitochondrial transmembrane potential disruption.
Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor.

Cell Viability Assay

Cell Line: HCS cells
Concentration: 294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM
Incubation Time: 4 hours, 8 hours, and 12 hours, 16 hours, 20 hours, 24 hours, 28 hours
Result: Decreased the viability of HCS cells with concentration and time at concentrations above 588.93 μM.

Apoptosis Analysis

Cell Line: HCS cells
Concentration: 294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM
Incubation Time: 4 hours, 8 hours, and 12 hours
Result: Induced apoptosis of HCS cells.

Cell Cycle Analysis

Cell Line: HCS cells
Concentration: 4.71 mM
Incubation Time: 4 hours, 8 hours, and 12 hours
Result: Arrested HCS cells at the G1 phase of the cell cycle.

Western Blot Analysis

Cell Line: HCS cells
Concentration: 4.71 mM
Incubation Time: 4 hours, 8 hours, and 12 hours
Result: Down-regulated the expression level of anti-apoptotic protein Bcl-xL and up-regulated the pro-apoptotic protein Bax, whereas significantly up-regulated the cytoplasmic amounts of mitochondria-released cytochrome C and apoptosis-inducing factor (AIF).
体内研究

Proparacaine Hydrochloride (75 μg/30 μL; intranasal administration; for 7 days) significantly decreases nasal symptoms, number of eosinophils, goblet cells, and mast cells in the lamina propria of the nasal mucosa.

Animal Model: 7-week-old female BALB/c mice, allergic rhinitis model
Dosage: 75 μg/30 μL
Administration: Intranasal administration, for 7 days
Result: Significantly reduced nasal rubbing and sneezing.
分子式
C16H26N2O3.HCl
分子量
330.85
CAS号
5875-06-9
中文名称
盐酸丙美卡因
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (151.13 mM; Need ultrasonic)

H2O : 33.33 mg/mL (100.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0225 mL 15.1126 mL 30.2252 mL
5 mM 0.6045 mL 3.0225 mL 6.0450 mL
10 mM 0.3023 mL 1.5113 mL 3.0225 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。-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: PBS

    Solubility: 60 mg/mL (181.35 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.56 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。

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.56 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。

  • 4.

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

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.56 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。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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