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.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 152273-12-6
- Formula: C17H21N3O2
- Molecular Weight:299.37
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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.
Chemical Information
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CAS No. 152273-12-6
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Appearance Solid
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Molecular Weight 299.37
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 Related Classifications
HY-100686 Related Classifications
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