1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. EP2 receptor agonist 2

EP2 receptor agonist 2 (compound 18a) is a potent and selective G protein-biased EP2 receptor agonist (hEP2G protein EC50 = 13 nM, hEP2β arrestin EC50 > 10000 nM). EP2 receptor agonist 2 exhibits excellent selectivity over hEP1/3/4, hIP and hFP (EC50s > 10000 nM).

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EP2 receptor agonist 2

EP2 receptor agonist 2 Chemical Structure

CAS No. : 1807780-00-2

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Description

EP2 receptor agonist 2 (compound 18a) is a potent and selective G protein-biased EP2 receptor agonist (hEP2G protein EC50 = 13 nM, hEP2β arrestin EC50 > 10000 nM). EP2 receptor agonist 2 exhibits excellent selectivity over hEP1/3/4, hIP and hFP (EC50s > 10000 nM)[1].

IC50 & Target[1]

EP2

13 nM (EC50)

hEP1

>10000 nM (EC50)

hEP3

>10000 nM (EC50)

hEP4

>10000 nM (EC50)

hFP

>10000 nM (EC50)

hIP

>10000 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
>10 μM
Compound: 18a
Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
[PMID: 26985320]
CHO EC50
13 nM
Compound: 1
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
[PMID: 27055938]
CHO EC50
13 nM
Compound: 18a
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
[PMID: 26985320]
HEK293 EC50
>10 μM
Compound: 1
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
[PMID: 27055938]
HEK293 EC50
>10 μM
Compound: 18a
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
[PMID: 26985320]
Molecular Weight

375.44

Formula

C19H21NO5S

CAS No.
SMILES

OC(C1=CSC([C@@H](CC2)O[C@](C[C@H]3O)([H])[C@@]2([H])[C@H]3COC4=CC=CC=C4)=N1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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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.

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Product Name:
EP2 receptor agonist 2
Cat. No.:
HY-128496
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