Gaboxadol hydrochloride
Based on 1 publication(s) in Google Scholar
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
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- Pureté : 99.90%
- CAS No.: 85118-33-8
- Formule: C6H9ClN2O2
- Masse moléculaire:176.60
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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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Publications Citing Use of MedChemExpress (MCE) Gaboxadol hydrochloride
More
Activité biologique
Description
IC50 & Target
GABAA receptor; GABAC receptor[1]
In Vitro
Gaboxadol hydrochloride (0.34, 3.5 and 7.0 μM) decreses permeability across Caco-2 cell monolayers with a dose dependent manner, shows the mean Papp values with 8.1 × 10-6 cm·s-1, 6.1 × 10-1 cm·s-6 and 5.6 × 10-6 cm·s-1 for 0.34, 3.5 and 7 μM gaboxadol, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fmr1 KO2 mice (deletion of the promoter and first exon of Fmr1 resulting in mRNA and protein null mice)[2]
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Dosage:0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg
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Administration:Intraperitoneal injection
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Result:Normalized Hyperactivity Observed in Fmr1 KO2 mice.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 85118-33-8
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Appearance Solid
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Masse moléculaire 176.60
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Formule C6H9ClN2O2
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Color White to off-white
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SMILES
O=C1C2=C(CNCC2)ON1.Cl
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Synonyms
Lu 02-030 hydrochloride; THIP hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Can J Physiol Pharmacol
2020 Oct;98(10):725-732. PMID: 32516556
Solvant et solubilité
In Vitro:
H2O : ≥ 100 mg/mL (566.25 mM)
DMSO : 75 mg/mL (424.69 mM; Need ultrasonic; 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 1.47 mg/mL (8.32 mM); Clear solution
This protocol yields a clear solution of ≥ 1.47 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.7 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: ≥ 1.47 mg/mL (8.32 mM); Clear solution
This protocol yields a clear solution of ≥ 1.47 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.7 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (566.25 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Johnston GA, et al. Neurochemicals for the investigation of GABA(C) receptors. Neurochem Res. 2010 Dec;35(12):1970-7. [Content Brief]
[2]. Cogram P, et al. Gaboxadol Normalizes Behavioral Abnormalities in a Mouse Model of Fragile X Syndrome.Front Behav Neurosci. 2019 Jun 25;13:141. [Content Brief]
[3]. Larsen M, et al. Intestinal gaboxadol absorption via PAT1 (SLC36A1): modified absorption in vivo following co-administration of L-tryptophan.Br J Pharmacol. 2009 Aug;157(8):1380-9. [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 (sealed storage, away from moisture and light). 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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.6625 mL | 28.3126 mL | 56.6251 mL | 141.5628 mL |
| 5 mM | 1.1325 mL | 5.6625 mL | 11.3250 mL | 28.3126 mL | |
| 10 mM | 0.5663 mL | 2.8313 mL | 5.6625 mL | 14.1563 mL | |
| 15 mM | 0.3775 mL | 1.8875 mL | 3.7750 mL | 9.4375 mL | |
| 20 mM | 0.2831 mL | 1.4156 mL | 2.8313 mL | 7.0781 mL | |
| 25 mM | 0.2265 mL | 1.1325 mL | 2.2650 mL | 5.6625 mL | |
| 30 mM | 0.1888 mL | 0.9438 mL | 1.8875 mL | 4.7188 mL | |
| 40 mM | 0.1416 mL | 0.7078 mL | 1.4156 mL | 3.5391 mL | |
| 50 mM | 0.1133 mL | 0.5663 mL | 1.1325 mL | 2.8313 mL | |
| 60 mM | 0.0944 mL | 0.4719 mL | 0.9438 mL | 2.3594 mL | |
| 80 mM | 0.0708 mL | 0.3539 mL | 0.7078 mL | 1.7695 mL | |
| 100 mM | 0.0566 mL | 0.2831 mL | 0.5663 mL | 1.4156 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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