1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Proparacaine hydrochloride

Proparacaine hydrochloride  (Synonyms: Proxymetacaine hydrochloride)

製品番号: HY-66012 純度: 99.87%
COA 取扱説明書 Technical Support

Proparacaine (Proxymetacaine) hydrochloride is a local anesthetic. Proparacaine hydrochloride blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine hydrochloride blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine hydrochloride is used in research related to cataracts.

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Proparacaine hydrochloride

Proparacaine hydrochloride 構造式

CAS 番号 : 5875-06-9

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
100 mg $25 在庫あり
500 mg $50 在庫あり
1 g $75 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

Other Forms of Proparacaine hydrochloride:

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製品説明

Proparacaine (Proxymetacaine) hydrochloride is a local anesthetic. Proparacaine hydrochloride blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine hydrochloride blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine hydrochloride is used in research related to cataracts[1][2][3].

体外実験

Proparacaine hydrochloride competitively inhibits the activity of 6-phosphogluconate dehydrogenase (6PGD) purified from human erythrocytes, with an IC50 of 601.60 μM and a Ki of 811.50 μM[1].
Proparacaine hydrochloride non-competitively inhibits the activity of glutathione reductase (GR) purified from human erythrocytes, with an IC50 of 686.90 μM and a Ki of 1,654.00 μM[1].
Proparacaine hydrochloride alters the actin cytoskeleton of corneal epithelial cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Proparacaine (0.20-2.92 μmol/kg; s.c.; single injection) hydrochloride induces dose-dependent cutaneous antinociception in rats with an ED50 of 0.57 μmol/kg, and coadministration with Dopamine (HY-B0451) produces a synergistic antinociceptive effect that enhances both the magnitude and duration of block[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 205-255 g)[3]
Dosage: 0.20, 0.44, 0.59, 1.17, and 2.92 μmol/kg
Administration: s.c.; single injection; i.p. (single injection, no effect)
Result: Produced dose-dependent cutaneous antinociception.
Induced 46% maximal possible effect (% MPE) of nociceptive block at ED50 dose.
Induced 100% MPE (complete nociceptive block in all 8 rats) when coadministered at 1/2 ED50 with dopamine 1/2 ED50.
Showed synergistic antinociceptive interaction with dopamine via isobolographic analysis: experimental ED50 of the combination (14.0 μmol/kg, 95% CI 12.5-15.6) was significantly lower than theoretical additive ED50.
Produced no cutaneous antinociceptive effects when administered i.p. at 2.92 μmol/kg alone or coadministered with dopamine at 1/2 ED50.
分子量

330.85

分子式

C16H27ClN2O3

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCN(CC)CC)C1=CC=C(OCCC)C(N)=C1.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (151.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

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体積 (開始)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.87%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.0225 mL 15.1126 mL 30.2252 mL 75.5629 mL
5 mM 0.6045 mL 3.0225 mL 6.0450 mL 15.1126 mL
10 mM 0.3023 mL 1.5113 mL 3.0225 mL 7.5563 mL
15 mM 0.2015 mL 1.0075 mL 2.0150 mL 5.0375 mL
20 mM 0.1511 mL 0.7556 mL 1.5113 mL 3.7781 mL
25 mM 0.1209 mL 0.6045 mL 1.2090 mL 3.0225 mL
30 mM 0.1008 mL 0.5038 mL 1.0075 mL 2.5188 mL
40 mM 0.0756 mL 0.3778 mL 0.7556 mL 1.8891 mL
50 mM 0.0605 mL 0.3023 mL 0.6045 mL 1.5113 mL
60 mM 0.0504 mL 0.2519 mL 0.5038 mL 1.2594 mL
80 mM 0.0378 mL 0.1889 mL 0.3778 mL 0.9445 mL
100 mM 0.0302 mL 0.1511 mL 0.3023 mL 0.7556 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Proparacaine hydrochloride
製品番号:
HY-66012
数量:
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