Gabapentin enacarbil

CAS No. 478296-72-9

Gabapentin enacarbil ( XP-13512 )

Catalog No. M26692 CAS No. 478296-72-9

Gabapentin enacarbil is a prodrug for the anticonvulsant and analgesic drug gabapentin.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 162 Get Quote
10MG 267 Get Quote
25MG 436 Get Quote
50MG 653 Get Quote
100MG Get Quote Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Gabapentin enacarbil
  • Note
    Research use only, not for human use.
  • Brief Description
    Gabapentin enacarbil is a prodrug for the anticonvulsant and analgesic drug gabapentin.
  • Description
    Gabapentin enacarbil 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) . (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%) .
  • Synonyms
    XP-13512
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    478296-72-9
  • Formula Weight
    329.4
  • Molecular Formula
    C16H27NO6
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CC(C)C(=O)OC(C)OC(=O)NCC1(CC(O)=O)CCCCC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Lingxiao Zhang, et al. Synthetic method of 3',5' -dichloro-2, 2, 2-trifluoro acetophenone derivative. CN113024390A
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