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Art. -Nr.: HY-189454

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ETK-III-9

ETK-III-9 is an orally active and blood-brain barrier-penetrant GABA_A receptor ligand. ETK-III-9 displaces ³H-flunitrazepam at the benzodiazepine site of GABA_A 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 GABA_A receptors and 7.6 nM for rat α5β3γ2 subtypes. ETK-III-9 is used in anxiety research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₁H₁₈BrFN₄O₂
Molecular Weight:457.30

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ETK-III-9 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

GABAA

97.8 nM (IC₅₀)

α5β3γ2

7.6 nM (IC₅₀)

In Vitro

Anti-cancerOthers

Anti-cancer

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].

Others

ETK-III-9 (Serially diluted ETK-III-9; 90 min) binds to rat brain GABA_A 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 GABA_A receptor subtypes at 100 nM^[1].
ETK-III-9 (1 nM to 1 μM; 90 min) binds to the α5β3γ2 GABA_A 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.

Cell Viability Assay^[1]

Cell Line:

HEK293T
Concentration:

300 μM
Incubation Time:

18 h
Result:

Showed no cellular toxicity up to 150 μM.
Reduced viability by 25% at 300 μM.
Exhibited an LD₅₀ higher than 300 μM.

Parmacokinetics

Species	Dose	Route	Note	T_max	C_max	T_1/2
Mice^[1]	40 mg/kg	p.o.	blood	120 min	11928 nM	234 min
Mice^[1]	40 mg/kg	p.o.	brain	120 min	10924 nM	209 min

In Vivo

ETK-III-9 (40 mg/kg; p.o.; single administration; 60 min before testing) does not alter locomotor activity or induce sedation in the open field test^[1].
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.

Animal Model:

Swiss Webster mice (female, 8-10 weeks old, 20-25 g)^[1]
Dosage:

40 mg/kg
Administration:

p.o.; single dose; 60 min before testing
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.

Animal Model:

Swiss Webster mice (female, 8-10 weeks old, 20-25 g)^[1]
Dosage:

40 mg/kg
Administration:

p.o.; single dose; 60 min before testing
Result:

Three out of ten ETK-III-9-treated mice did not complete the rotarod test.

Animal Model:

Swiss Webster mice (female, 8-10 weeks old, 20-25 g)^[1]
Dosage:

40 mg/kg
Administration:

p.o.; single dose; 60 min before testing
Result:

Had profound effects on mouse behavior, with a significant reduction in buried marbles.

Chemical Information

Molecular Weight 457.30
Formel C₂₁H₁₈BrFN₄O₂
SMILES

BrC1=CC=C(C2=C1)N3C(C(C)N=C2C4=CC=CC=C4F)=C(C(NCCO)=O)N=C3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Toriola MA, et al. Development of Novel Pegylated Imidazobenzodiazepines Targeting α5 GABAA Receptors for Anxiety: A Comparative Prodrug and Metabolite Study. ACS chemical neuroscience. 2026 Sep 02;17(17):3181-3191.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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