| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
U-93631 targets the GABAA receptor, a ligand-gated ion channel responsible for mediating inhibitory neurotransmission in the central nervous system. It binds to the picrotoxin site and stabilizes the receptor/channel complex in an inactivated state. It also inhibits 5-HT3A receptors via a similar mechanism.
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| ln Vitro |
In vitro, U-93631 accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude in HEK293 cells expressing rat α1β2, β2γ2, and α1γ2 subunit-containing GABAA receptors. It induces a rapid, time-dependent decay of GABA-induced whole-cell Cl- currents in recombinant GABAA receptors. When used at a concentration of 5 μM, it accelerates decay of GABA-induced currents.
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| ln Vivo |
In vivo, U-93631 acts as a GABAA receptor antagonist. By stabilizing the inactive form of the channel, it reduces GABAergic neurotransmission. Its effects have been studied in various preclinical models of neurological disorders.
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| Enzyme Assay |
In vitro receptor binding assays for U-93631 typically use membrane preparations from cells expressing GABAA receptors. Radiolabeled ligands that bind to the picrotoxin site are displaced by increasing concentrations of the compound to determine binding affinity. Functional assays measure the compound's ability to modulate GABA-induced chloride currents using patch-clamp electrophysiology. U-93631 has an IC50 of 100 nM.
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| Cell Assay |
Cell-based functional assays for U-93631 involve measuring GABA-induced chloride currents in cells expressing GABAA receptors. Whole-cell patch-clamp recordings are used to measure currents in the presence and absence of the compound. The compound's ability to accelerate current decay is quantified.
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| Animal Protocol |
In vivo animal studies for U-93631 typically involve administration to animal models to study its effects on the central nervous system. Its ability to modulate GABAergic neurotransmission and its effects on behavior, seizure activity, and other neurological endpoints are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of U-93631 are characteristic of small molecule GABAA receptor modulators. The compound has a molecular weight of 299.37 and a molecular formula of C17H21N3O2. It is typically dissolved in DMSO for in vitro experiments.
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| Toxicity/Toxicokinetics |
The toxicological profile of U-93631 has been evaluated in preclinical studies. As a GABAA receptor antagonist, it can cause central nervous system effects. Its safety profile is consistent with other compounds that modulate GABAergic neurotransmission.
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| References |
: Dillon GH, Im HK, Hamilton BJ, Carter DB, Gammill RB, Judge TM, Im WB. U-93631 causes rapid decay of gamma-aminobutyric acid-induced chloride currents in recombinant rat gamma-aminobutyric acid type A receptors. Mol Pharmacol. 1993 Oct;44(4):860-5. PubMed PMID: 8232235.
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| Additional Infomation |
U-93631 is a GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel. It is a valuable research tool for studying GABAA receptor function and GABAergic neurotransmission. It is not approved for clinical use.
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| Molecular Formula |
C17H21N3O2
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|---|---|
| Molecular Weight |
299.367543935776
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| Exact Mass |
299.163
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| CAS # |
152273-12-6
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| Related CAS # |
152273-12-6;
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| PubChem CID |
197626
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| Appearance |
White to off-white solid powder
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| Density |
1.19g/cm3
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| Boiling Point |
470.1ºC at 760 mmHg
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| Flash Point |
238.1ºC
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| Vapour Pressure |
5.2E-09mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
3.626
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
444
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NXBSEJKZKXIYMD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21N3O2/c1-16(2,3)22-15(21)13-14-17(4,5)19-11-8-6-7-9-12(11)20(14)10-18-13/h6-10,19H,1-5H3
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| Chemical Name |
tert-butyl 4,4-dimethyl-5H-imidazo[1,5-a]quinoxaline-3-carboxylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ≥ 34 mg/mL (~113.57 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3403 mL | 16.7017 mL | 33.4035 mL | |
| 5 mM | 0.6681 mL | 3.3403 mL | 6.6807 mL | |
| 10 mM | 0.3340 mL | 1.6702 mL | 3.3403 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.
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