2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. HZ166

HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects. HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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HZ166 Chemical Structure

HZ166 Chemical Structure

CAS No. : 612527-56-7

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HZ166 Related Antibodies

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Description

HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects[1]. HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
> 20 μM
Compound: 2; HZ-166
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
[PMID: 27933953]
HEK293 EC50
0.844 μM
Compound: 2; HZ-166
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
[PMID: 27933953]
Molecular Weight

356.38

Formula

C21H16N4O2
CAS No.
SMILES

O=C(OCC)C1=C2N(C3=CC=C(C=C3C(C4=NC=CC=C4)=NC2)C#C)C=N1
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HZ166 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HZ166612527-56-7HZ 166HZ-166GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα2-GABAA receptorsα3-GABAA receptorsanti-hyperalgesic effectsInhibitorinhibitorinhibit

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HY-123249
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