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Gabapentin enacarbil

Gabapentin enacarbil
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Gabapentin enacarbil

Catalog No. T15366Cas No. 478296-72-9
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. Gabapentin enacarbil provides sustained dose-proportional exposure to gabapentin and predictable bioavailability.
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Product Introduction

Bioactivity
Description
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. Gabapentin enacarbil provides sustained dose-proportional exposure to gabapentin 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].
AliasXP-13512
Chemical Properties
Molecular Weight329.39
FormulaC16H27NO6
Cas No.478296-72-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: 95 mg/mL (288.41 mM)
DMSO: 95 mg/mL (288.41 mM)
H2O: 0.6 mg/mL (1.82 mM)
Solution Preparation Table
Ethanol/H2O
1mg5mg10mg50mg
1 mM3.0359 mL15.1796 mL30.3591 mL151.7957 mL
Ethanol
1mg5mg10mg50mg
5 mM0.6072 mL3.0359 mL6.0718 mL30.3591 mL
10 mM0.3036 mL1.5180 mL3.0359 mL15.1796 mL
20 mM0.1518 mL0.7590 mL1.5180 mL7.5898 mL
50 mM0.0607 mL0.3036 mL0.6072 mL3.0359 mL
100 mM0.0304 mL0.1518 mL0.3036 mL1.5180 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
1 Enter information below:
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