| 常用名 | 1-[[[[1-(2-甲基-1-氧代丙氧基)乙氧基]甲酰]氨基]甲基]环己烷乙酸 | CAS号 | 478296-72-9 |
|---|---|---|---|
| 价格 | $需询单/100g $需询单/1kg $需询单/100kg $需询单/1000kg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情(用途,包装等)
用途: Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.IC50 Value: Target: Calcium ChannelGabapentin enacarbil is an actively transported prodrug of gabapentin that provides sustained dose-proportional exposure to gabapentin and predictable bioavailability.in vitro: The prodrug (XP-13512) 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 XP13512 immediate- and extended-release formulations were compared with those of oral gabapentin. XP13512 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 物理化学性质: CAS号:478296-72-9 常用中文名:1-[[[[1-(2-甲基-1-氧代丙氧基)乙氧基]甲酰]氨基]甲基]环己烷乙酸 常用英文名:Gabapentin enacarbil 分子式:C16H27NO6 分子量:329.389 密度:1.1±0.1 g/cm3 沸点:482.0±20.0 °C at 760 mmHg 熔点:65ºC 闪点:245.3±21.8 °C 储存条件:2-8℃ |