THIP
Based on 1 publication(s) in Google Scholar
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
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- 純度: 99.89%
- CAS 番号: 64603-91-4
- 分子式: C6H8N2O2
- 分子量:140.14
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 THIP
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生物活性
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α4β3δ GABAAR 13 μM (EC50) |
THIP (1 μM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons[1].
THIP (1 μM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)
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Concentration:1 µM
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Incubation Time:5 s
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Result:Induced a tonic current of 43.2 pA.
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Cell Line:Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)
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Concentration:1 µM
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Incubation Time:1 s
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Result:Resulted in only minor changes in the amplitude and frequency of mIPSCs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (255-276 g)[2].
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Dosage:2.5 mg/kg (for i.v.); 0.5 and 5.0 mg/kg (for p.o.).
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Administration:Oral gavage; intravenous injection; single.
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Result:
1.19 Pharmacokinetic Parameters of THIP 4 in Sprague-Dawley rats[2].
IV (2.5 mg/kg) PO (0.5 mg/kg) PO (5.0 mg/kg) AUC (ng/mL•h) 1193 263 1988 Tmax (h) - 0.22 0.33 Cmax (ng/mL) 4350 291 2061 CL/Fa (mL/h/kg) - 1939 2558 CL (mL/h/kg) 2043 - - Fa (%) 100 110 83
化学情報
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CAS 番号 64603-91-4
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性状 Solid
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分子量 140.14
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分子式 C6H8N2O2
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Color White to yellow
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SMILES
O=C1C2=C(CNCC2)ON1
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別名
Gaboxadol
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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
溶剤 & 溶解度
DMSO : 50 mg/mL (356.79 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 23.33 mg/mL (166.48 mM; Need ultrasonic)
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. 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. 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (17.84 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: ≥ 2.08 mg/mL (14.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 50 mg/mL (356.79 mM); Clear solution; Need ultrasonic
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.
純度とドキュメンテーション
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データシート (281 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Drasbek KR, et al. THIP, a hypnotic and antinociceptive drug, enhances an extrasynaptic GABAA receptor-mediated conductance in mouse neocortex. Cereb Cortex. 2006 Aug;16(8):1134-41. [Content Brief]
[2]. Larsen M, et al. 5-Hydroxy-L-tryptophan alters gaboxadol pharmacokinetics in rats: involvement of PAT1 and rOat1 in gaboxadol absorption and elimination. Eur J Pharm Sci. 2010 Jan 31;39(1-3):68-75. [Content Brief]
[3]. Hoestgaard-Jensen K, et al. Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain. J Neurosci. 2014 Dec 3;34(49):16256-72. [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. 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 7.1357 mL | 35.6786 mL | 71.3572 mL | 178.3930 mL |
| 5 mM | 1.4271 mL | 7.1357 mL | 14.2714 mL | 35.6786 mL | |
| 10 mM | 0.7136 mL | 3.5679 mL | 7.1357 mL | 17.8393 mL | |
| 15 mM | 0.4757 mL | 2.3786 mL | 4.7571 mL | 11.8929 mL | |
| 20 mM | 0.3568 mL | 1.7839 mL | 3.5679 mL | 8.9197 mL | |
| 25 mM | 0.2854 mL | 1.4271 mL | 2.8543 mL | 7.1357 mL | |
| 30 mM | 0.2379 mL | 1.1893 mL | 2.3786 mL | 5.9464 mL | |
| 40 mM | 0.1784 mL | 0.8920 mL | 1.7839 mL | 4.4598 mL | |
| 50 mM | 0.1427 mL | 0.7136 mL | 1.4271 mL | 3.5679 mL | |
| 60 mM | 0.1189 mL | 0.5946 mL | 1.1893 mL | 2.9732 mL | |
| 80 mM | 0.0892 mL | 0.4460 mL | 0.8920 mL | 2.2299 mL | |
| 100 mM | 0.0714 mL | 0.3568 mL | 0.7136 mL | 1.7839 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.
THIP 関連分類
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