JY-XHe-053
JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors.
For research use only. We do not sell to patients.
- CAS No.: 612526-36-0
- Formula: C22H16FN3O2
- Molecular Weight:373.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>20 μM
Compound: 3; JY-Xhe-053
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Binding affinity to human GABAA alpha1beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
Binding affinity to human GABAA alpha1beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
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[PMID: 27933953] |
| HEK293 | EC50 |
0.029 μM
Compound: 3; JY-Xhe-053
|
Binding affinity to human GABAA alpha3beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
Binding affinity to human GABAA alpha3beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
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[PMID: 27933953] |
Chemical Information
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CAS No. 612526-36-0
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Molecular Weight 373.38
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Formula C22H16FN3O2
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SMILES
O=C(OCC)C1=C2CN=C(C3=CC(C#C)=CC=C3N2C=N1)C4=CC=CC=C4F
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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
[1]. Rivas FM, Stables JP, Murphree L, et al. Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. J Med Chem. 2009;52(7):1795-1798. [Content Brief]
[2]. Savić MM, Majumder S, Huang S, et al. Novel positive allosteric modulators of GABAA receptors: do subtle differences in activity at alpha1 plus alpha5 versus alpha2 plus alpha3 subunits account for dissimilarities in behavioral effects in rats?. Prog Neuropsychopharmacol Biol Psychiatry. 2010;34(2):376-386. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JY-XHe-053 Related Classifications
HY-123426 Related Classifications
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