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Prilocaine (Synonyms: Propitocaine, NSC 40027, Citanest)

Name: Prilocaine
Brand: TargetMol
SKU: T6953
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T6953 Copy Product Info

Purity: 98.49%

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Prilocaine (NSC-40027) is a local anesthetic of the amino amide type, which acts on the sodium channel on the neuronal membrane and limits the spread of seizures.

Prilocaine

Copy Product Info

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Catalog No. T6953

Synonyms Propitocaine, NSC 40027, Citanest

Prilocaine (NSC-40027) is a local anesthetic of the amino amide type, which acts on the sodium channel on the neuronal membrane and limits the spread of seizures.

Cas No. 721-50-6

Pack Size	Price	USA Stock	Global Stock
25 mg	$30	In Stock	In Stock
50 mg	$40	In Stock	In Stock
100 mg	$64	In Stock	In Stock
200 mg	$93	In Stock	In Stock
500 mg	$155	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$44	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.49%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Prilocaine AI Summary

Prilocaine is an agent showing significant bioactivity against neuronal voltage-gated sodium channels by displacing [3H]BTX-B from high-affinity sites, with IC50 values ranging from 53,700 nM to as low as 1.73 nM depending on the assay conditions. It also inhibits binding related to the toxin Batrachotoxin in guinea pig cerebral cortex vesicles. The compound demonstrates variable inhibitory effects, with 14.2% inhibition at 10 µM and 58.5% inhibition at 100 µM concentrations. It has been observed to impact Histone Lysine Methyltransferase G9a, HP1-beta Chromodomain, and ATXN expression, while enhancing Arylsulfatase A (ASA1), displaying potencies between 301.3 nM and 31,622.8 nM. Pharmacokinetically, Prilocaine shows a log P value range of 2.12 to 2.3, indicating moderate lipophilicity. It exhibits a dissociation constant, with pKa values around 7.8 to 7.9, and a variable log K value depending on pH levels. In humans, after intravenous administration, it does not bind extensively to plasma proteins (logFu=0.715), and has a volume of distribution at steady state (Vdss) of 3.7 L.kg-1, a clearance rate of 29.0 mL.min-1.kg-1, and a half-life of 1.8 hours. Following topical application, it shows a Tmax ranging from 0.35 to 10 hours and Cmax values between 2.5 and 635.44 nM. In additional bioactivity assays, Prilocaine demonstrates a range of activities, including inhibition against human HDAC6, antiviral activity against SARS-CoV-2 in VERO-6 cells (IC50 > 19952.62 nM), and a mix of agonist and antagonist activities at multiple human receptors such as PPARG, CHRM1, HTR2B, and ADRB2. Moreover, it exhibits mixed results in inhibition assays, showing inconsistent activity across different substrates..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Prilocaine (NSC-40027) is a local anesthetic of the amino amide type, which acts on the sodium channel on the neuronal membrane and limits the spread of seizures.
Synonyms	Propitocaine, NSC 40027, Citanest

Chemical Properties

Molecular Weight	220.31
Formula	C₁₃H₂₀N₂O
Cas No.	721-50-6
Smiles	CCCNC(C)C(=O)Nc1ccccc1C
Relative Density.	1.0117 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 41 mg/mL (186.1 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 45 mg/mL (204.26 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (9.08 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.5391 mL	22.6953 mL	45.3906 mL	226.9529 mL
5 mM	0.9078 mL	4.5391 mL	9.0781 mL	45.3906 mL
10 mM	0.4539 mL	2.2695 mL	4.5391 mL	22.6953 mL
20 mM	0.2270 mL	1.1348 mL	2.2695 mL	11.3476 mL
50 mM	0.0908 mL	0.4539 mL	0.9078 mL	4.5391 mL
100 mM	0.0454 mL	0.2270 mL	0.4539 mL	2.2695 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc