1. GPCR/G Protein
  2. Arrestin Apelin Receptor (APJ)
  3. APJ receptor agonist 6

APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively.

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APJ receptor agonist 6 Chemical Structure

APJ receptor agonist 6 Chemical Structure

CAS No. : 1965244-85-2

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Description

APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively[1].

IC50 & Target

EC50: 0.800 ± 0.1 μM (Apelin Receptor calcium), 0.844 ± 0.2 μM (Apelin Receptor cAMP), 6.22 ± 2.0 μM (Apelin Receptor β-arrestin), >10 μM (AT1 calcium)[1]

Cellular Effect
Cell Line Type Value Description References
CHO EC50
> 10 μM
Compound: 9
Agonist activity at human AGTR1 stably expressed in CHO cells assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 sec by calcium 5 dye based FLIPR assay
Agonist activity at human AGTR1 stably expressed in CHO cells assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 sec by calcium 5 dye based FLIPR assay
[PMID: 31948845]
CHO EC50
0.8 μM
Compound: 9
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
[PMID: 31948845]
CHO EC50
0.844 μM
Compound: 9
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
[PMID: 31948845]
CHO-K1 EC50
3406 nM
Compound: 22
Partial agonist activity at rat NTS2 receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
Partial agonist activity at rat NTS2 receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
[PMID: 27369451]
CHO-K1 EC50
6.22 μM
Compound: 9
Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
[PMID: 31948845]
Molecular Weight

523.60

Formula

C29H34FN3O5

CAS No.
SMILES

COC1=CC=CC(OC)=C1C2=CC(C(N[C@H](CC(O)=O)CCC3CCCCC3)=O)=NN2C4=CC=C(C=C4)F

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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APJ receptor agonist 6 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.

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Product Name:
APJ receptor agonist 6
Cat. No.:
HY-147751
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