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

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

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Gabapentin hydrochloride Chemical Structure

Gabapentin hydrochloride Chemical Structure

CAS No. : 60142-95-2

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Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
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100 mg USD 90 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Gabapentin hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

In Vitro

Gabapentin (0-300 μM) hydrochloride 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) hydrochloride decreases the K+-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively[1]. Gabapentin (0-1000 μM) hydrochloride 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.

In Vivo

Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) hydrochloride 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) hydrochloride 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

207.70

Formula

C9H18ClNO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1(CN)CCCCC1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (240.73 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8146 mL 24.0732 mL 48.1464 mL
5 mM 0.9629 mL 4.8146 mL 9.6293 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 10 mg/mL (48.15 mM); Clear solution; Need ultrasonic

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%

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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
H2O 1 mM 4.8146 mL 24.0732 mL 48.1464 mL 120.3659 mL
5 mM 0.9629 mL 4.8146 mL 9.6293 mL 24.0732 mL
10 mM 0.4815 mL 2.4073 mL 4.8146 mL 12.0366 mL
15 mM 0.3210 mL 1.6049 mL 3.2098 mL 8.0244 mL
20 mM 0.2407 mL 1.2037 mL 2.4073 mL 6.0183 mL
25 mM 0.1926 mL 0.9629 mL 1.9259 mL 4.8146 mL
30 mM 0.1605 mL 0.8024 mL 1.6049 mL 4.0122 mL
40 mM 0.1204 mL 0.6018 mL 1.2037 mL 3.0091 mL
50 mM 0.0963 mL 0.4815 mL 0.9629 mL 2.4073 mL
60 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0061 mL
80 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5046 mL
100 mM 0.0481 mL 0.2407 mL 0.4815 mL 1.2037 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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  • 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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Gabapentin hydrochloride
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