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Gabapentin enacarbil

Name: Gabapentin enacarbil
Brand: TargetMol
SKU: T15366
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15366Cas No. 478296-72-9

Alias XP-13512

Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic gabapentin, offering sustained dose-proportional exposure and predictable bioavailability.

Gabapentin enacarbil

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Purity: 99.31%

Catalog No. T15366Alias XP-13512Cas No. 478296-72-9

Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic gabapentin, offering sustained dose-proportional exposure and predictable bioavailability.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$35	-	In Stock
5 mg	$81	In Stock	In Stock
10 mg	$129	In Stock	In Stock
25 mg	$289	-	In Stock
50 mg	$463	-	In Stock
100 mg	$742	-	In Stock
200 mg	$987	-	In Stock
1 mL x 10 mM (in DMSO)	$89	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.31%

Appearance:Oil

Color:Transparent

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic gabapentin, offering sustained dose-proportional exposure and predictable bioavailability.
In vitro	Gabapentin enacarbil demonstrated active apical to basolateral transport across Caco-2 cell monolayers and pH-dependent passive permeability across artificial membranes. XP13512 inhibited uptake of (14)C-lactate by human embryonic kidney cells expressing monocarboxylate transporter type-1, and direct uptake of prodrug by these cells was confirmed using liquid chromatography-tandem mass spectrometry. XP13512 inhibited uptake of (3)H-biotin into Chinese hamster ovary cells overexpressing human sodium-dependent multivitamin transporter (SMVT) [1].
In vivo	In 4 studies of healthy volunteers (136 subjects total), the pharmacokinetics of Gabapentin enacarbil immediate- and extended-release formulations were compared with those of oral gabapentin. Gabapentin enacarbil immediate-release (up to 2800 mg single dose and 2100 mg twice daily) was well absorbed (>68%, based on urinary recovery of gabapentin), converted rapidly to gabapentin, and provided dose-proportional exposure, whereas absorption of oral gabapentin declined with increasing doses to <27% at 1200 mg. Compared with 600 mg gabapentin, an equimolar Gabapentin enacarbil extended-release dose provided extended gabapentin exposure (time to maximum concentration, 8.4 vs 2.7 hours) and superior bioavailability (74.5% vs 36.6%) [2].
Synonyms	XP-13512

Chemical Properties

Molecular Weight	329.39
Formula	C₁₆H₂₇NO₆
Cas No.	478296-72-9
Smiles	CC(C)C(=O)OC(C)OC(=O)NCC1(CC(O)=O)CCCCC1
Relative Density.	1.134

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 95 mg/mL (288.41 mM), Sonication is recommended.

DMSO: 95 mg/mL (288.41 mM), Sonication is recommended.

H2O: 0.6 mg/mL (1.82 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (10.02 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0359 mL	15.1796 mL	30.3591 mL	151.7957 mL

Ethanol/DMSO

	1mg	5mg	10mg	50mg
5 mM	0.6072 mL	3.0359 mL	6.0718 mL	30.3591 mL
10 mM	0.3036 mL	1.5180 mL	3.0359 mL	15.1796 mL
20 mM	0.1518 mL	0.7590 mL	1.5180 mL	7.5898 mL
50 mM	0.0607 mL	0.3036 mL	0.6072 mL	3.0359 mL
100 mM	0.0304 mL	0.1518 mL	0.3036 mL	1.5180 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc