1. Bupivacaine

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.

Bupivacaine Chemical Structure

Bupivacaine Chemical Structure

CAS No. : 38396-39-3

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

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Description

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[1][2][3].

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.
Clinical Trial
Molecular Weight

288.43

Formula

C18H28N2O

CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4670 mL 17.3352 mL 34.6705 mL
5 mM 0.6934 mL 3.4670 mL 6.9341 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, 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.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.92%

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, 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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  • 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.

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Bupivacaine
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