Gabapentin enacarbil
Based on 1 Customer Validation
Gabapentin enacarbil (XP-13512) is a prodrug of Gabapentin (HY-A0057) designed to be absorbed throughout the intestine by high-capacity nutrient transporters. Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin enacarbil can be used for the study of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
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- Pureté: 99.90%
- CAS No.: 478296-72-9
- Formule: C16H27NO6
- Masse moléculaire:329.39
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Stockage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Gabapentin enacarbil (XP-13512) demonstrates active apical to basolateral transport across Caco-2 cell monolayers and pH-dependent passive permeability across artificial membranes[1].
Gabapentin enacarbil inhibits uptake of 14C-lactate by human embryonic kidney cells expressing monocarboxylate transporter type-1[1].
Gabapentin enacarbil inhibits uptake of 3H-biotin into Chinese hamster ovary cells overexpressing human sodium-dependent multivitamin transporter (SMVT)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In rats, >95% of an oral dose of 14C-Gabapentin enacarbil is excreted in urine in 24 h as Gabapentin[2].
In monkeys, oral bioavailability of Gabapentin from Gabapentin enacarbil capsules was 84.2%[2].
Compared with intracolonic Gabapentin, intracolonic Gabapentin enacarbil gave a 17-fold higher Gabapentin exposure in rats and 34-fold higher in monkeys[2].
Gabapentin enacarbil may therefore be incorporated into a sustained release formulation to provide extended Gabapentin exposure. Gabapentin enacarbil demonstrates improved Gabapentin bioavailability, increases dose proportionality, and enhances colonic absorption[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 478296-72-9
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Appearance Oil
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Masse moléculaire 329.39
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Formule C16H27NO6
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Color Light yellow to brown
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SMILES
O=C(O)CC1(CNC(OC(OC(C(C)C)=O)C)=O)CCCCC1
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Synonyms
XP-13512
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvant et solubilité
Ethanol : 100 mg/mL (303.59 mM; Need ultrasonic)
DMSO : ≥ 100 mg/mL (303.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Cundy KC, et al. XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pharmacol Exp Ther. 2004 Oct;311(1):315-23. [Content Brief]
[2]. Cundy KC, et al. XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 3.0359 mL | 15.1796 mL | 30.3591 mL | 75.8979 mL |
| 5 mM | 0.6072 mL | 3.0359 mL | 6.0718 mL | 15.1796 mL | |
| 10 mM | 0.3036 mL | 1.5180 mL | 3.0359 mL | 7.5898 mL | |
| 15 mM | 0.2024 mL | 1.0120 mL | 2.0239 mL | 5.0599 mL | |
| 20 mM | 0.1518 mL | 0.7590 mL | 1.5180 mL | 3.7949 mL | |
| 25 mM | 0.1214 mL | 0.6072 mL | 1.2144 mL | 3.0359 mL | |
| 30 mM | 0.1012 mL | 0.5060 mL | 1.0120 mL | 2.5299 mL | |
| 40 mM | 0.0759 mL | 0.3795 mL | 0.7590 mL | 1.8974 mL | |
| 50 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.5180 mL | |
| 60 mM | 0.0506 mL | 0.2530 mL | 0.5060 mL | 1.2650 mL | |
| 80 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9487 mL | |
| 100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.7590 mL |
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