Art. -Nr.: HY-A0079

Tetracaine

(Synonyms: Amethocaine)

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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.

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Reinheit: 99.87%
CAS. Nr.: 94-24-6
Formel: C₁₅H₂₄N₂O₂
Molecular Weight:264.36

Speicherung:

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

Tetracaine Chemical Structure

CAS. Nr.: 94-24-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 94-24-6
Appearance Solid
Molecular Weight 264.36
Formel C₁₅H₂₄N₂O₂
Color White to off-white
SMILES

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

Amethocaine
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Journal Impact Factor

JACC Basic Transl Sci

JP2 and JCN Crosstalk Abrogate MURF1-Mediated JCN Ubiquitination and Degradation in Cardiomyocytes. [Abstract]

2026 Apr 17;11(5):101534. PMID: 42000606

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Tetracaine

1 Cited Publications

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Tetracaine

Publications Citing Use of MedChemExpress (MCE) Tetracaine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tetracaine Related Classifications

HY-A0079 Related Classifications