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Fig. 1 · Structure
Cat. No.
A13215
CAS No.
217082-60-5
Formula
C69H108N22O16S
Mol. Weight
1533.81

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(Glp1)-Apelin-13

Cat. No. A13215 CAS 217082-60-5

Apelin Receptor activator

(Glp1)-Apelin-13 is an activator of Apelin Receptor

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
CHO EC50 0.0003 μM 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 EC50 0.002 μM 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-K1 EC50 0.001 μM 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]
HEK293 EC50 0.047 nM Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay [PMID: 31724863]
HEK293 EC50 0.062 nM Agonist activity at rat APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay [PMID: 31724863]
HEK293 EC50 0.84 nM Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay [PMID: 25668242]
HEK293 EC50 1.1 nM Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay [PMID: 29461833]
HEK293 IC50 1.2 nM Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting method [PMID: 25668242]
HEK293 EC50 1.4 nM Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay [PMID: 25668242]
HEK293 EC50 12.2 pM Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay [PMID: 25241924]
HEK293 EC50 24 nM Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA [PMID: 29461833]
HEK293 EC50 26 nM Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated for 30 mins by BRET assay [PMID: 25668242]
HEK293 EC50 29 nM Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay [PMID: 25668242]
HEK293 EC50 5.9 nM Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of GalphaoA subunit dissociation incubated for 5 mins by BRET assay [PMID: 25668242]
HEK293 EC50 60 nM Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay [PMID: 29461833]

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Specifications

Manufacturer Adooq Bioscience
Actions Activator
CAS Number 217082-60-5
Applications Apelin Receptor activator
Formula C69H108N22O16S
Molecular Weight 1533.81
Synonyms [Pyr1]-Apelin-13
SMILES
CC(C)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@@H](CCSC)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]6CCC(=O)N6

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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