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Proparacaine HCl Sodium Channel antagonist

Name: Proparacaine HCl
Brand: Selleck Chemicals
SKU: S1828
Rating: 5 (1 reviews)

Cat.No.S1828

Proparacaine HCl (Proxymetacaine Hydrochloride) is a voltage-gated Sodium Channel antagonist with ED50 of 3.4 mM.

Chemical Structure

Molecular Weight: 330.85

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Quality Control

Batch: S182801 Water]66 mg/mL]false]DMSO]12 mg/mL]false]Ethanol]Insoluble]false Purity: 99.60%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.60

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Sodium Channel Inhibitors	Camostat Mesilate A-803467 cariporide Tolperisone HCl Vinpocetine Veratramine Bulleyaconi cine A Ambroxol HCl Benzocaine Nefopam HCl

Chemical Information, Storage & Stability

Molecular Weight	330.85	Formula	C₁₆H₂₆N₂O₃.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	5875-06-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Proxymetacaine Hydrochloride			Smiles	CCCOC1=C(C=C(C=C1)C(=O)OCCN(CC)CC)N.Cl

Solubility

In vitro
Batch:

Water : 66 mg/mL

DMSO : 12 mg/mL (36.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (90.68mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Voltage-gated sodium channel 3.4 mM(ED50)
In vitro	Proparacaine is more potent and less toxic than cocaine. Proparacaine significantly increases in FHV-1 (P < 0.01), C. felis, and 28S rDNA Ct values when fusidic acid is used.
In vivo	Proparacaine inhibits corneal epithelial migration and adhesion through alteration of the actin cytoskeleton. Proparacaine acts like bupivacaine or lidocaine and produces dose-related spinal blockades of motor function, proprioception and nociception. Intrathecal proxymetacaine also produces longer sensory blockade than motor blockade.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7925683/ [2] https://pubmed.ncbi.nlm.nih.gov/21923818/ [3] https://pubmed.ncbi.nlm.nih.gov/3198982/ [4] https://pubmed.ncbi.nlm.nih.gov/19429093/

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