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U93631

U93631
GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.
Catalog No. T3644Cas No. 152273-12-6
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Purity:99.76%
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U93631

Catalog No. T3644Cas No. 152273-12-6
GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.
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Pack SizePriceAvailabilityQuantity
10 mg$29In Stock
25 mg$64In Stock
50 mg$98In Stock
100 mg$173In Stock
200 mg$257In Stock
1 mL x 10 mM (in DMSO)$29In Stock
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Product Introduction

Bioactivity
Description
GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.
Targets&IC50
GABAA:100 nM
In vitro
In the presence of U93631 at 5 UM, the peak amplitude decreased as a function of GABA concentration, with the half-maximal inhibitory concentration being approximately 100 nM, which is close to the Kd for the high affinity GABA site(85 nM). It appears that the drug interacts with GABA-bound receptors (at least monoliganded) and accelerates receptor desensitization, rather than acting as an open channel blocker.
Chemical Properties
Molecular Weight299.37
FormulaC17H21N3O2
Cas No.152273-12-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (183.72 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3403 mL16.7017 mL33.4035 mL167.0174 mL
5 mM0.6681 mL3.3403 mL6.6807 mL33.4035 mL
10 mM0.3340 mL1.6702 mL3.3403 mL16.7017 mL
20 mM0.1670 mL0.8351 mL1.6702 mL8.3509 mL
50 mM0.0668 mL0.3340 mL0.6681 mL3.3403 mL
100 mM0.0334 mL0.1670 mL0.3340 mL1.6702 mL

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