Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gabapentin enacarbil (XP-13512) 是抗惊厥和镇痛药物加巴喷丁的前药。Gabapentin enacarbil 提供持续剂量比例的 Gabapentin 暴露和可预测的生物利用度。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,070 | 5日内发货 | ||
25 mg | ¥ 4,140 | 6-8周 | ||
50 mg | ¥ 5,380 | 6-8周 | ||
100 mg | ¥ 8,120 | 6-8周 |
产品描述 | 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. |
体外活性 | 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]. |
体内活性 | 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]. |
别名 | XP-13512, 加巴喷丁酯 |
分子量 | 329.39 |
分子式 | C16H27NO6 |
CAS No. | 478296-72-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO / H2O | 1 mM | 3.0359 mL | 15.1796 mL | 30.3591 mL | 75.8979 mL |
Ethanol / DMSO | 5 mM | 0.6072 mL | 3.0359 mL | 6.0718 mL | 15.1796 mL |
10 mM | 0.3036 mL | 1.518 mL | 3.0359 mL | 7.5898 mL | |
20 mM | 0.1518 mL | 0.759 mL | 1.518 mL | 3.7949 mL | |
50 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.518 mL | |
100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.759 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Gabapentin enacarbil 478296-72-9 Membrane transporter/Ion channel Metabolism Others Calcium Channel XP-13512 inhibit XP 13512 Inhibitor Ca channels XP13512 加巴喷丁酯 Ca2+ channels inhibitor