Tetracaine (Synonyms: Amethocaine)

Name: Tetracaine
Brand: MedChemExpress
SKU: HY-A0079
Rating: 4.5 (1 reviews)

Cat. No.: HY-A0079 Purity: 99.87%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Tetracaine (Amethocaine) is a sodium channel inhibitor and ryanodine receptor (RyR) inhibitor. Tetracaine blocks sodium conduction across nerve cell membranes, preventing rapid sodium ion influx and depolarization. Tetracaine exhibits biphasic effects on spontaneous sarcoplasmic reticulum Ca²⁺ release in Ca²⁺-overloaded ventricular myocytes, and increases sarcoplasmic reticulum Ca²⁺ load. Tetracaine can be used in research related to eye diseases.

For research use only. We do not sell to patients.

Tetracaine Chemical Structure

CAS No. : 94-24-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	Get quote
50 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tetracaine:

Tetracaine hydrochloride In-stock
Tetracaine (Standard) Get quote

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

View All Calcium Channel Isoform Specific Products:

View All Isoforms

N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	0.53 μM Compound: tetracaine	Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
CHO-K1	IC₅₀	1.1 μM Compound: tetracaine	Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	0.11 μM Compound: tetracaine	Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	0.49 μM Compound: Tetracaine	Inhibition of recombinant human Nav1.2 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay Inhibition of recombinant human Nav1.2 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay	[PMID: 27015369]
HEK293	IC₅₀	0.52 μM Compound: Tetracaine	Inhibition of recombinant human Nav1.6 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay Inhibition of recombinant human Nav1.6 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay	[PMID: 27015369]
HEK293	IC₅₀	0.62 μM Compound: tetracaine	Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	0.65 μM Compound: Tetracaine	Inhibition of human Nav1.5 expressed in HEK293 cells by whole cell-patch clamp method Inhibition of human Nav1.5 expressed in HEK293 cells by whole cell-patch clamp method	[PMID: 27015369]
HEK293	IC₅₀	0.74 μM Compound: Tetracaine	Inhibition of recombinant human Nav1.3 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay Inhibition of recombinant human Nav1.3 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay	[PMID: 27015369]
HEK293	IC₅₀	33 μM Compound: tetracaine	Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	7.51 μM Compound: Tetracaine	Inhibition of human NaV1.7 expressed in HEK293 cells by [14C]guanidinium influx assay Inhibition of human NaV1.7 expressed in HEK293 cells by [14C]guanidinium influx assay	[PMID: 21570288]

In Vitro

Tetracaine inhibits human NaV1.7 channel with IC₅₀ values of 0.11 μM (V_hold = -65 mV) and 0.62 μM (V_hold = -90 mV), respectively, and shows >300-fold reduced potency against the NaV1.7^F1737A mutant channel^[1].
Tetracaine (V_hold = -90 mV) inhibits human NaV1.5 channel with an IC₅₀ value of 0.53 μM^[1].
Tetracaine (V_hold = -65 mV) inhibits human NaV1.2 channel with an IC₅₀ value of 1.1 μM^[1].
Tetracaine exerts biphasic effects on spontaneous Ca²⁺ release in Ca²⁺-overloaded rat ventricular myocytes, initially inhibiting Ca²⁺ sparks and waves at concentrations >0.25 mM, then potentiating release at submaximal concentrations (<1.25 mM), while completely abolishing release at ≥1.5 mM^[3].
Tetracaine (0.75 mM; 2-5 min) causes a time-dependent increase in SR Ca²⁺ load in Ca²⁺-overloaded rat ventricular myocytes, with a 19% increase after 2 min and a 54% increase after 5 min of exposure^[3].
Tetracaine (0.75 mM; up to 10 min) has delayed potentiation of spontaneous Ca²⁺ release in rat ventricular myocytes that depends on extracellular Ca²⁺ concentration^[3].
Tetracaine (1 mM) enhances net Ca²⁺ uptake in isolated canine cardiac SR microsomes by reducing Ca²⁺ leakage through RyR channels^[3].
Tetracaine inhibits canine cardiac SR RyR channel activity in planar lipid bilayers with an EC₅₀ of 0.26 mM at low luminal Ca²⁺, and this inhibition is reversed by elevated luminal Ca²⁺^[3].

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

Clinical Trial

Molecular Weight

264.36

Formula

C₁₅H₂₄N₂O₂

CAS No.

94-24-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCN(C)C)C1=CC=C(NCCCC)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 43 mg/mL (162.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7827 mL	18.9136 mL	37.8272 mL
5 mM	0.7565 mL	3.7827 mL	7.5654 mL
10 mM	0.3783 mL	1.8914 mL	3.7827 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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 (9.46 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 (9.46 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (276 KB) SDS (644 KB)

COA (242 KB) HNMR (167 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Macsari I, et al. 3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models. J Med Chem. 2012;55(15):6866-6880. [Content Brief]

[2]. Bartfield JM, et al. A comparison of proparacaine and tetracaine eye anesthetics. Acad Emerg Med. 1994;1(4):364-367.

[3]. Györke S, et al. Dual effects of tetracaine on spontaneous calcium release in rat ventricular myocytes. J Physiol. 1997;500 ( Pt 2)(Pt 2):297-309.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.7827 mL	18.9136 mL	37.8272 mL	94.5680 mL
	5 mM	0.7565 mL	3.7827 mL	7.5654 mL	18.9136 mL
	10 mM	0.3783 mL	1.8914 mL	3.7827 mL	9.4568 mL
	15 mM	0.2522 mL	1.2609 mL	2.5218 mL	6.3045 mL
	20 mM	0.1891 mL	0.9457 mL	1.8914 mL	4.7284 mL
	25 mM	0.1513 mL	0.7565 mL	1.5131 mL	3.7827 mL
	30 mM	0.1261 mL	0.6305 mL	1.2609 mL	3.1523 mL
	40 mM	0.0946 mL	0.4728 mL	0.9457 mL	2.3642 mL
	50 mM	0.0757 mL	0.3783 mL	0.7565 mL	1.8914 mL
	60 mM	0.0630 mL	0.3152 mL	0.6305 mL	1.5761 mL
	80 mM	0.0473 mL	0.2364 mL	0.4728 mL	1.1821 mL
	100 mM	0.0378 mL	0.1891 mL	0.3783 mL	0.9457 mL

Tetracaine Related Classifications

Neurological Disease

Help & FAQs

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.

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Tetracaine (Synonyms: Amethocaine)

Customer Review

Other Forms of Tetracaine:

Tetracaine Related Antibodies

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

View All Calcium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tetracaine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tetracaine Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report