U93631
Based on 1 Customer Validation
U93631 is a GABAA receptor inhibitor targeting the picrotoxin (HY-101391) site, which exhibits higher inhibitory potency in receptors lacking α subunits. U93631 blocks GABA-induced chloride currents, exerts a mild initial stimulatory effect on activated currents, but its activity decreases in β2T246F mutant receptors. U93631 can serve as a ligand for the convulsant site of GABAA receptors in relevant studies.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.85%
- CAS 番号: 152273-12-6
- 分子式: C17H21N3O2
- 分子量:299.37
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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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Help & FAQs
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生物活性
U93631 (200 nM GABA) exhibits higher affinity for both single-ligand and multi-ligand recombinant rat α1β2γ2 GABAa receptors expressed in HEK293 cells than for resting-state receptors, and its efficacy in blocking Cl− currents increases after pre-incubation with 200 nM GABA[1].
U93631 (0.5-50 μM; 10 s) inhibits GABA-activated Cl− currents in HEK293 cells expressing α2β2γ2 GABAA receptors, with an IC50 of 4.9 μM; it also induces mild initial current stimulation at concentrations of 2 μM and 5 μM[2].
U93631 (20 μM; 5 min) blocks the binding of picrotoxin to the binding sites on α3β2γ2 and α6β2γ2 GABAA receptors expressed in HEK293 cells, which is confirmed by the accelerated current recovery rate following picrotoxin exposure[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 152273-12-6
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性状 Solid
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分子量 299.37
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分子式 C17H21N3O2
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Color White to off-white
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SMILES
O=C(C1=C2N(C=N1)C3=C(C=CC=C3)NC2(C)C)OC(C)(C)C
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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 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : ≥ 34 mg/mL (113.57 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dillon GH, et al. Enhancement by GABA of the association rate of picrotoxin and tert-butylbicyclophosphorothionate to the rat cloned alpha 1 beta 2 gamma 2 GABAA receptor subtype. Br J Pharmacol. 1995 Jun;115(3):539-45. [Content Brief]
[2]. Bell-Horner CL, et al. Influence of subunit configuration on the interaction of picrotoxin-site ligands with recombinant GABA(A) receptors. Brain Res Mol Brain Res. 2000;76(1):47-55. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3403 mL | 16.7017 mL | 33.4035 mL | 83.5087 mL |
| 5 mM | 0.6681 mL | 3.3403 mL | 6.6807 mL | 16.7017 mL | |
| 10 mM | 0.3340 mL | 1.6702 mL | 3.3403 mL | 8.3509 mL | |
| 15 mM | 0.2227 mL | 1.1134 mL | 2.2269 mL | 5.5672 mL | |
| 20 mM | 0.1670 mL | 0.8351 mL | 1.6702 mL | 4.1754 mL | |
| 25 mM | 0.1336 mL | 0.6681 mL | 1.3361 mL | 3.3403 mL | |
| 30 mM | 0.1113 mL | 0.5567 mL | 1.1134 mL | 2.7836 mL | |
| 40 mM | 0.0835 mL | 0.4175 mL | 0.8351 mL | 2.0877 mL | |
| 50 mM | 0.0668 mL | 0.3340 mL | 0.6681 mL | 1.6702 mL | |
| 60 mM | 0.0557 mL | 0.2784 mL | 0.5567 mL | 1.3918 mL | |
| 80 mM | 0.0418 mL | 0.2088 mL | 0.4175 mL | 1.0439 mL | |
| 100 mM | 0.0334 mL | 0.1670 mL | 0.3340 mL | 0.8351 mL |
U93631 関連分類
HY-100686 関連分類
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