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Gabapentin enacarbil
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
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.
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Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | XP-13512 |
| Molecular Weight | 329.39 |
| Formula | C16H27NO6 |
| Cas No. | 478296-72-9 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 95 mg/mL (288.41 mM), Sonication is recommended. DMSO: 95 mg/mL (288.41 mM) H2O: 0.6 mg/mL (1.82 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
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(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 DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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