ETK-III-9
ETK-III-9 is an orally active and blood-brain barrier-penetrant GABAA receptor ligand. ETK-III-9 displaces 3H-flunitrazepam at the benzodiazepine site of GABAA receptors, with stronger interactions at α3β3γ2 and α5β3γ2 subtypes. ETK-III-9 exhibits a target IC50 value of 97.8 nM for rat α3/α5-containing GABAA receptors and 7.6 nM for rat α5β3γ2 subtypes. ETK-III-9 is used in anxiety research.
For research use only. We do not sell to patients.
- Formula: C21H18BrFN4O2
- Molecular Weight:457.30
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
GABAA 97.8 nM (IC50) |
α5β3γ2 7.6 nM (IC50) |
In Vitro
ETK-III-9 (300 μM; 18 h) shows no cytotoxicity up to 150 μM and has an LD50 greater than 300 μM in HEK293T cells[1].
ETK-III-9 (Serially diluted ETK-III-9; 90 min) binds to rat brain GABAA receptors with an IC50 of 97.8 nM[1].
ETK-III-9 (Serially diluted ETK-III-9; 90 min) exhibits weak affinity for the kappa opioid receptor with an IC50 of 1.59 μM[1].
ETK-III-9 (100 nM; 90 min) interacts strongly with α3β3γ2 and α5β3γ2 GABAA receptor subtypes at 100 nM[1].
ETK-III-9 (1 nM to 1 μM; 90 min) binds to the α5β3γ2 GABAA receptor with an IC50 of 7.6 nM[1].
ETK-III-9 (10 μM; 2 h) is metabolically stable toward phase I metabolism in mouse liver microsomes with 88.2% remaining after 2 h[1].
ETK-III-9 (10 μM; 2 h) is metabolically stable toward phase II (glucuronidation) metabolism with 96.1% remaining after 2 h[1].
ETK-III-9 (10 μM; 4 h) has a free plasma fraction of 9.7% in mouse plasma[1].
ETK-III-9 (10 μM; 4 h) has a free brain fraction (fu) of 6.6% in mouse brain homogenate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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:Showed no cellular toxicity up to 150 μM.
Reduced viability by 25% at 300 μM.
Exhibited an LD50 higher than 300 μM.
Parmacokinetics
In Vivo
ETK-III-9 (40 mg/kg; p.o.; single administration; 60 min before testing) produces anxiolytic-like effects in the elevated plus maze, increasing the time spent in the open arms without altering locomotor activity[1].
ETK-III-9 (40 mg/kg; p.o.; single administration; 60 min before testing) produces partial sensorimotor impairment in the rotarod test (3/10 mice fail)[1].
ETK-III-9 (40 mg/kg; p.o.; single administration; 60 min before testing) significantly reduces marble-burying behavior, indicating anxiolytic-like activity[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 mice (female, 8-10 weeks 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:Did not influence overall behavior of mice.
No changes were observed in total distance traveled, average speed, maximum speed, total time freezing, total time mobile, and total time immobile compared to vehicle-treated mice.\n
Did not change total distance traveled.
Spent significantly more time in the open zone (anxiolysis) and less time in the closed zone compared to vehicle.
Open arm entries and head dips were not statistically different from vehicle controls.
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Animal Model:Swiss Webster mice (female, 8-10 weeks 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:Three out of ten ETK-III-9-treated mice did not complete the rotarod test.
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Animal Model:Swiss Webster mice (female, 8-10 weeks 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:Had profound effects on mouse behavior, with a significant reduction in buried marbles.
Chemical Information
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Molecular Weight 457.30
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Formula C21H18BrFN4O2
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SMILES
BrC1=CC=C(C2=C1)N3C(C(C)N=C2C4=CC=CC=C4F)=C(C(NCCO)=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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ETK-III-9 Related Classifications
HY-189454 Related Classifications
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