2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Gabapentin

Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain.

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

Gabapentin Chemical Structure

Gabapentin Chemical Structure

CAS No. : 60142-96-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Gabapentin:

Gabapentin Related Antibodies

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

  • Biological Activity

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  • References

  • Customer Review

Description

Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain[1][2][3].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
30 μM
Compound: 1
Inhibition of [3H]leucine uptake into CHO cells by L-amino acid transporters
Inhibition of [3H]leucine uptake into CHO cells by L-amino acid transporters
[PMID: 15801823]
In Vitro

Gabapentin (0-300 μM) produces a concentration-dependent inhibition of the K+-induced [Ca2+]i increase in synaptosomes (IC50=14?μM; maximal inhibition by 36%)[1].
? Gabapentin (100? μM) decreases the K+-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively[1].
? Gabapentin (0-1000 μM) reduces the K+-evoked [3H]-noradrenaline release in neocortical slices (IC50=48?μM; maximal inhibition of 46%) but not from synaptosomes[1].

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

Gabapentin Related Antibodies
In Vivo

Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) has improving effects on spatial and emotional cognitive performance of naive mice in Morris water maze (MWM), passive avoidance (PA) and modified elevated plus maze (mEPM) tasks[2].
? Gabapentin (1-100 mg/kg; i.p.; once; male mice) has analgesic effect and reduces writhing in a dose-dependent manner[3].

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

Animal Model: Male BALB/c mice (35-45 g)[2]
Dosage: 5 and 10 mg/kg
Administration: Intraperitoneal injection; once
Result: Increased the time spent in target quadrant and decreased the distance to platform in MWM test
. Decreased the transfer latency on second day in mEPM test
. Prolonged retention latency in PA test
.
Animal Model: Male mice (26-30 g)[3]
Dosage: 1, 5, 10, 50 and 100 mg/kg
Administration: Intraperitoneal injection; once
Result: Produced 45-70% inhibition of writhing.
Clinical Trial
Molecular Weight

171.24

Formula

C9H17NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1(CN)CCCCC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (291.99 mM; Need ultrasonic)

DMSO : 1 mg/mL (5.84 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 5.8398 mL 29.1988 mL 58.3976 mL
5 mM 1.1680 mL 5.8398 mL 11.6795 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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=
Concentration (final)

C2

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In Vivo:

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:  PBS

    Solubility: 25 mg/mL (145.99 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

SDS (557 KB)

COA (251 KB) HNMR (234 KB) MS (69 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 5.8398 mL 29.1988 mL 58.3976 mL 145.9939 mL
5 mM 1.1680 mL 5.8398 mL 11.6795 mL 29.1988 mL
H2O 10 mM 0.5840 mL 2.9199 mL 5.8398 mL 14.5994 mL
15 mM 0.3893 mL 1.9466 mL 3.8932 mL 9.7329 mL
20 mM 0.2920 mL 1.4599 mL 2.9199 mL 7.2997 mL
25 mM 0.2336 mL 1.1680 mL 2.3359 mL 5.8398 mL
30 mM 0.1947 mL 0.9733 mL 1.9466 mL 4.8665 mL
40 mM 0.1460 mL 0.7300 mL 1.4599 mL 3.6498 mL
50 mM 0.1168 mL 0.5840 mL 1.1680 mL 2.9199 mL
60 mM 0.0973 mL 0.4866 mL 0.9733 mL 2.4332 mL
80 mM 0.0730 mL 0.3650 mL 0.7300 mL 1.8249 mL
100 mM 0.0584 mL 0.2920 mL 0.5840 mL 1.4599 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Gabapentin Related Classifications

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.

Keywords:

Gabapentin60142-96-3Calcium ChannelCa2+ channelsCa channelsCa2+neurotransmitterGABA analogneuropathic painInhibitorinhibitorinhibit

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