Cat. No.: HY-B0405A

Bupivacaine hydrochloride

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.

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

Purity: 99.85%
CAS No.: 18010-40-7
Formula: C₁₈H₂₉ClN₂O
Molecular Weight:324.89

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Bupivacaine hydrochloride Chemical Structure

CAS No.: 18010-40-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

NMDA Receptor

All iGluR Isoforms :

All Sodium Channel Isoforms :

All Calcium Channel Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	22 μM Compound: (R,S)-bupivacaine	Inhibition of wild-type human ERG channel expressed in CHO cells by whole-cell patch clamp technique Inhibition of wild-type human ERG channel expressed in CHO cells by whole-cell patch clamp technique	[PMID: 21624711]
CHO	IC₅₀	95 μM Compound: (R,S)-bupivacaine	Inhibition of human ERG Y652A mutant channel expressed in CHO cells by whole-cell patch clamp technique Inhibition of human ERG Y652A mutant channel expressed in CHO cells by whole-cell patch clamp technique	[PMID: 21624711]
HEK293	IC₅₀	265 μM Compound: (R,S)-bupivacaine	Inhibition of human ERG Y652A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique Inhibition of human ERG Y652A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique	[PMID: 21624711]
HEK293	IC₅₀	32 μM Compound: (R,S)-bupivacaine	Inhibition of wild-type human ERG channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique Inhibition of wild-type human ERG channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique	[PMID: 21624711]
HEK293	IC₅₀	866 μM Compound: (R,S)-bupivacaine	Inhibition of human ERG F656A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique Inhibition of human ERG F656A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique	[PMID: 21624711]

In Vitro

Bupivacaine hydrochloride inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization^[1].
Bupivacaine hydrochloride influences the voltage dependency of channel activation and steady-state inactivation by shifting the membrane potential of half-maximal activation/inactivation toward somewhat more negative membrane potentials. In their inactivated state, SCN5A channels are slightly sensitive toward Bupivacaine hydrochloride IC₅₀=2.18±0.16 μM^[2].
Bupivacaine hydrochloride reversibly inhibits the SK2 channel in a dose-dependent manner with the IC ₅₀ of 16.5 μM^[3].

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

Cell Viability Assay^[3]

Cell Line:

HEK 293 cells transfected with the SK2 gene (transfected cells were named SK2 cells)
Concentration:

10, 100, 1000 µM
Incubation Time:
Result:

The IC₅₀ value was 16.5 µM.

Clinical Trial

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

Chemical Information

CAS No. 18010-40-7
Appearance Solid
Molecular Weight 324.89
Formula C₁₈H₂₉ClN₂O
Color White to off-white
SMILES

O=C(C1N(CCCC)CCCC1)NC2=C(C)C=CC=C2C.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Publications (4)

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Journal Impact Factor

Cell

Cancer cells co-opt an inter-organ neuroimmune circuit to escape immune surveillance. [Abstract]

2025 Nov 26;188(24):6754-6773.e29. PMID: 41138728
Nat Commun

Structural mapping of Nav1.7 antagonists. [Abstract]

2023 Jun 3;14(1):3224. PMID: 37270609
Sci Adv

EphB1-NR2B receptor signaling in glutamatergic neurons of the ventroposteromedial thalamic nucleus regulates emergence from anesthesia. [Abstract]

2025 Dec 5;11(49):eadw7972. PMID: 41348875
Stem Cell Res Ther

Local anesthetics impair the growth and self-renewal of glioblastoma stem cells by inhibiting ZDHHC15-mediated GP130 palmitoylation. [Abstract]

2021 Feb 4;12(1):107. PMID: 33541421

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (76.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

3.0780 mL

15.3898 mL

30.7796 mL

5 mM

0.6156 mL

3.0780 mL

6.1559 mL

10 mM

0.3078 mL

1.5390 mL

3.0780 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (7.69 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.69 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.

Working Solution

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: 50% PEG300 50% PBS

Solubility: 12.5 mg/mL (38.47 mM); Clear solution; Need ultrasonic

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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)

References

[1]. Casati A, et, al. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different? Best Pract Res Clin Anaesthesiol. 2005 Jun;19(2):247-68. [Content Brief]

[2]. Dan J, et, al. Inhibition of gastric cancer by local anesthetic bupivacaine through multiple mechanisms independent of sodium channel blockade. Biomed Pharmacother. 2018 Jul;103:823-828. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0780 mL	15.3898 mL	30.7796 mL	76.9491 mL
	5 mM	0.6156 mL	3.0780 mL	6.1559 mL	15.3898 mL
	10 mM	0.3078 mL	1.5390 mL	3.0780 mL	7.6949 mL
	15 mM	0.2052 mL	1.0260 mL	2.0520 mL	5.1299 mL
	20 mM	0.1539 mL	0.7695 mL	1.5390 mL	3.8475 mL
	25 mM	0.1231 mL	0.6156 mL	1.2312 mL	3.0780 mL
	30 mM	0.1026 mL	0.5130 mL	1.0260 mL	2.5650 mL
	40 mM	0.0769 mL	0.3847 mL	0.7695 mL	1.9237 mL
	50 mM	0.0616 mL	0.3078 mL	0.6156 mL	1.5390 mL
	60 mM	0.0513 mL	0.2565 mL	0.5130 mL	1.2825 mL

Keywords

Bupivacaine hydrochloride

4 Cited Publications

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Bupivacaine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Bupivacaine hydrochloride

All iGluR Isoforms

All Sodium Channel Isoforms

All Calcium Channel Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bupivacaine hydrochloride Related Classifications

HY-B0405A Related Classifications