Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Gaboxadol ( Lu-02030, THIP, OV-101; Lu-02-030; MK-0928) is a potent GABA agonist. It is an agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50 = 25 μM). Gaboxadol can also be a non-opioid analgesic and a novel type of hypnotic.
ln Vitro |
The permeability of Caco-2 cell monolayers was lowered in a dose-dependent manner by gaboxadol hydrochloride (0.34, 3.5, and 7.0 μM), with mean Papp values of 8.1 × 10-6 cm·s-1, 6.1 × 10 -1 cm·s-1 for 0.34, 3.5, and 7 μM gaboxadol, and 5.6 × 10-6 cm·s-1 for 0.34, 3.5, and 7 μM gaboxadol, respectively[3].
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ln Vivo |
Gaboxadol hydrochloride (intraperitoneal injection; 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg; thrice daily; three days apart) normalizes walking distance in Fmr1 KO2 mice to 0.5 mg/kg WT activity level, in addition, the chemical had no effect on locomotor activity in Fmr1 KO2 mice [2].
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Animal Protocol |
Animal/Disease Models: Fmr1 KO2 mice (the Fmr1 promoter and first exon are deleted, resulting in mice with missing mRNA and protein) [2]
Doses: 0.5, 1, 1.5, 2, 3, 4 or 5 mg/kg given Medication: intraperitoneal (ip) injection Experimental Results: Normalized hyperactivity was observed in Fmr1 KO2 mice. |
References |
[1]. Johnston GA, et al. Neurochemicals for the investigation of GABA(C) receptors. Neurochem Res. 2010 Dec;35(12):1970-7.
[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. [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. |
Molecular Formula |
C6H9CLN2O2
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Molecular Weight |
176.6009
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CAS # |
85118-33-8
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Related CAS # |
THIP;64603-91-4
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SMILES |
O=C1NOC2=C1CCNC2.[H]Cl
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InChi Key |
ZDZDSZQYRBZPNN-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C6H8N2O2.ClH/c9-6-4-1-2-7-3-5(4)10-8-6/h7H,1-3H2,(H,8,9)1H
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Chemical Name |
4,5,6,7-Tetrahydroisoxazolo(5,4-c)pyridin-3(2H)-one monohydrochloride
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Synonyms |
OV-101 OV101Lu-02-030 MK-0928 MK 0928Lu-02030 OV 101 Lu02-030 MK0928 Lu02030. THIP
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~566.25 mM)
DMSO : ~75 mg/mL (~424.69 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.47 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.47 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.47 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (566.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 5.6625 mL | 28.3126 mL | 56.6251 mL | |
5 mM | 1.1325 mL | 5.6625 mL | 11.3250 mL | |
10 mM | 0.5663 mL | 2.8313 mL | 5.6625 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.