Cat. No.: HY-B0405

Bupivacaine

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Bupivacaine 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 can be used for the research of chronic pain.

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

Purity: 99.95%
CAS No.: 38396-39-3
Formula: C₁₈H₂₈N₂O
Molecular Weight:288.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bupivacaine Chemical Structure

CAS No.: 38396-39-3

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

Biological Activity

Description

IC₅₀ & Target

NMDA Receptor

All iGluR Isoforms :

All Sodium Channel Isoforms :

All Calcium Channel Isoforms :

In Vitro

Bupivacaine inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization^[1].
Bupivacaine 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 IC₅₀=2.18±0.16 μM^[2].
Bupivacaine 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.

Chemical Information

CAS No. 38396-39-3
Appearance Solid
Molecular Weight 288.43
Formula C₁₈H₂₈N₂O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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 : 100 mg/mL (346.70 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

3.4670 mL

17.3352 mL

34.6705 mL

5 mM

0.6934 mL

3.4670 mL

6.9341 mL

10 mM

0.3467 mL

1.7335 mL

3.4670 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.67 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 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]. Meaghan A Paganelli, et al. Actions of Bupivacaine, a widely used local anesthetic, on NMDA receptor responses. J Neurosci. 2015 Jan 14;35(2):831-42. [Content Brief]

[2]. Alexander P Schwoerer, et al. A Comparative Analysis of Bupivacaine and Ropivacaine Effects on Human Cardiac SCN5A Channels. Anesth Analg. 2015 Jun;120(6):1226-34. [Content Brief]

[3]. Carsten Stoetzer, et al. Inhibition of Voltage-Gated Na⁺ Channels by Bupivacaine Is Enhanced by the Adjuvants Buprenorphine, Ketamine, and Clonidine. Reg Anesth Pain Med.Jul/Aug 2017;42(4):462-468. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4670 mL	17.3352 mL	34.6705 mL	86.6761 mL
	5 mM	0.6934 mL	3.4670 mL	6.9341 mL	17.3352 mL
	10 mM	0.3467 mL	1.7335 mL	3.4670 mL	8.6676 mL
	15 mM	0.2311 mL	1.1557 mL	2.3114 mL	5.7784 mL
	20 mM	0.1734 mL	0.8668 mL	1.7335 mL	4.3338 mL
	25 mM	0.1387 mL	0.6934 mL	1.3868 mL	3.4670 mL
	30 mM	0.1156 mL	0.5778 mL	1.1557 mL	2.8892 mL
	40 mM	0.0867 mL	0.4334 mL	0.8668 mL	2.1669 mL
	50 mM	0.0693 mL	0.3467 mL	0.6934 mL	1.7335 mL
	60 mM	0.0578 mL	0.2889 mL	0.5778 mL	1.4446 mL
	80 mM	0.0433 mL	0.2167 mL	0.4334 mL	1.0835 mL
	100 mM	0.0347 mL	0.1734 mL	0.3467 mL	0.8668 mL

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Bupivacaine

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Publications Citing Use of MedChemExpress (MCE) Bupivacaine

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 Related Classifications

Cat. No.: HY-B0405