ETK-II-83
ETK-II-83 is an orally effective and blood-brain barrier-penetrant ligand for the benzodiazepine site of the GABAA receptor. ETK-II-83 displaces 3H-flunitrazepam from rat brain GABAA receptors and selectively binds to the α5-containing subtype. ETK-II-83 can be used for anxiety research.
For research use only. We do not sell to patients.
- Formula: C28H32BrFN4O5
- Molecular Weight:603.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
ETK-II-83 (300 μM; 18 h) shows no significant cytotoxicity in HEK293T cells up to 300 μM[1].
ETK-II-83 selectively binds α5-containing GABAA receptors with an IC50 of 18.3 nM[1].
ETK-II-83 (10 μM; 2 h) undergoes rapid phase I metabolism in mouse liver microsomes with a half-life of 5.33 min[1].
ETK-II-83 (10 μM; 4 h) has an unbound plasma fraction of 6.4% in mouse plasma[1].
ETK-II-83 (10 μM; 4 h) exhibits a free brain fraction of 12.7% in mouse brain homogenate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:HEK293T
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Concentration:300 μM
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Incubation Time:18 h
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Result:No cellular toxicity was observed up to a concentration of 150 μM.
A 25% reduction in viability was observed at 300 μM.
The LD50 of ETK-II-83 is higher than 300 μM.
Parmacokinetics
In Vivo
ETK-II-83 (40 mg/kg; p.o.; single administration; 60 min before testing) significantly reduces marble-burying behavior in mice, suggesting anxiolytic-like activity[1].
ETK-II-83 (40 mg/kg; p.o.; single administration; 60 min before testing) does not induce sedation or alter locomotor behavior in mice in the open field test[1].
ETK-II-83 (40 mg/kg; p.o.; single administration; 60 min before testing) does not impair sensorimotor coordination in mice in the rotarod test[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Webster (female, 8- to 10-week-old, 20−25 g)[1]
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Dosage:40 mg/kg
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Administration:p.o.; single dose; 60 min before testing
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Result:Increased time spent in the open zone and decreased time in the closed zone.
No significant differences in total distance traveled, open arm entries, or head dips.
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Animal Model:Swiss Webster (female, 8- to 10-week-old, 20−25 g)[1]
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Dosage:40 mg/kg
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Administration:p.o.; single dose; 60 min before testing
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Result:Significantly reduced buried marbles compared to vehicle control.
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Animal Model:Swiss Webster (female, 8- to 10-week-old, 20−25 g)[1]
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Dosage:40 mg/kg
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Administration:p.o.; single dose; 60 min before testing
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Result:No changes in total distance traveled, average speed, maximum speed, total time freezing, total time mobile, or total time immobile compared to vehicle-treated mice.
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Animal Model:Swiss Webster (female, 8- to 10-week-old, 20−25 g)[1]
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Dosage:40 mg/kg
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Administration:p.o.; single dose; 60 min before testing
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Result:All ETK-II-83-treated mice completed the 3 min rotarod task (n = 16).
Chemical Information
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Molecular Weight 603.48
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Formula C28H32BrFN4O5
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SMILES
BrC1=CC=C(C2=C1)N3C(C(C)N=C2C4=CC=CC=C4F)=C(C(NCCOCCOCCOCCOC)=O)N=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ETK-II-83 Related Classifications
HY-189453 Related Classifications
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