AY77
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.
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- CAS No.: 1835734-92-3
- Formule: C21H32N4O4
- Masse moléculaire:404.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
PAR2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
2 μM
Compound: 2; AY77
|
Agonist activity at PK1-tagged PAR2 (unknown origin) expressed in HEK293 cells assessed as induction of beta-arrestin recruitment incubated for 90 mins by Pathhunter chemiluminescent assay
Agonist activity at PK1-tagged PAR2 (unknown origin) expressed in HEK293 cells assessed as induction of beta-arrestin recruitment incubated for 90 mins by Pathhunter chemiluminescent assay
|
[PMID: 32551018] |
| HEK-293T | EC50 |
0.17 μM
Compound: 2; AY77
|
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
|
[PMID: 32551018] |
Chemical Information
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CAS No. 1835734-92-3
-
Masse moléculaire 404.50
-
Formule C21H32N4O4
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Sequence
{5-Isoxazolylcarbonyl-Cha}-{Chg}-NH2
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Sequence Shortening
{5-Isoxazolylcarbonyl-Cha}-{Chg}-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)