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

Gabapentin enacarbil  (Synonyms: XP-13512)

Cat. No.: HY-16216 Purity: ≥95.0%
SDS
COA
Handling Instructions Technical Support

Gabapentin enacarbil (XP-13512) is a prodrug of Gabapentin (HY-A0057) designed to be absorbed throughout the intestine by high-capacity nutrient transporters. Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin enacarbil can be used for the study of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).

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

Gabapentin enacarbil Chemical Structure

Gabapentin enacarbil Chemical Structure

CAS No. : 478296-72-9

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Oil
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Gabapentin enacarbil:

Gabapentin enacarbil 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

  • Purity & Documentation

  • References

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Description

Gabapentin enacarbil (XP-13512) is a prodrug of Gabapentin (HY-A0057) designed to be absorbed throughout the intestine by high-capacity nutrient transporters. Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin enacarbil can be used for the study of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN)[1][2].

In Vitro

Gabapentin enacarbil (XP-13512) demonstrates active apical to basolateral transport across Caco-2 cell monolayers and pH-dependent passive permeability across artificial membranes[1].
Gabapentin enacarbil inhibits uptake of 14C-lactate by human embryonic kidney cells expressing monocarboxylate transporter type-1[1].
Gabapentin enacarbil inhibits uptake of 3H-biotin into Chinese hamster ovary cells overexpressing human sodium-dependent multivitamin transporter (SMVT)[1].

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

Gabapentin enacarbil Related Antibodies
In Vivo

Gabapentin enacarbil (XP-13512) is stable at physiological pH but rapidly converted to gabapentin in intestinal and liver tissue from rats, dogs, monkeys, and humans[1].
In rats, >95% of an oral dose of 14C-Gabapentin enacarbil is excreted in urine in 24 h as Gabapentin[2].
In monkeys, oral bioavailability of Gabapentin from Gabapentin enacarbil capsules was 84.2%[2].
Compared with intracolonic Gabapentin, intracolonic Gabapentin enacarbil gave a 17-fold higher Gabapentin exposure in rats and 34-fold higher in monkeys[2].
Gabapentin enacarbil may therefore be incorporated into a sustained release formulation to provide extended Gabapentin exposure. Gabapentin enacarbil demonstrates improved Gabapentin bioavailability, increases dose proportionality, and enhances colonic absorption[2].

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

329.39

Formula

C16H27NO6
CAS No.
Appearance

Oil

Color

Light yellow to brown

SMILES

O=C(O)CC1(CNC(OC(OC(C(C)C)=O)C)=O)CCCCC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (303.59 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (303.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0359 mL 15.1796 mL 30.3591 mL
5 mM 0.6072 mL 3.0359 mL 6.0718 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

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 (7.59 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.59 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥95.0%

SDS (393 KB)

COA (246 KB) HNMR (340 KB) MS (70 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). 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
Ethanol / DMSO 1 mM 3.0359 mL 15.1796 mL 30.3591 mL 75.8979 mL
5 mM 0.6072 mL 3.0359 mL 6.0718 mL 15.1796 mL
10 mM 0.3036 mL 1.5180 mL 3.0359 mL 7.5898 mL
15 mM 0.2024 mL 1.0120 mL 2.0239 mL 5.0599 mL
20 mM 0.1518 mL 0.7590 mL 1.5180 mL 3.7949 mL
25 mM 0.1214 mL 0.6072 mL 1.2144 mL 3.0359 mL
30 mM 0.1012 mL 0.5060 mL 1.0120 mL 2.5299 mL
40 mM 0.0759 mL 0.3795 mL 0.7590 mL 1.8974 mL
50 mM 0.0607 mL 0.3036 mL 0.6072 mL 1.5180 mL
60 mM 0.0506 mL 0.2530 mL 0.5060 mL 1.2650 mL
80 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
100 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7590 mL
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Gabapentin enacarbil 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:

Gabapentin enacarbil478296-72-9XP-13512XP13512XP 13512Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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