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Cat. No.: HY-147751

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APJ receptor agonist 6

APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with K_i 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.

For research use only. We do not sell to patients.

CAS No.: 1965244-85-2
Formula: C₂₉H₃₄FN₃O₅
Molecular Weight:523.60

Storage:

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

Data Sheet (272 KB)

APJ receptor agonist 6 Chemical Structure

CAS No.: 1965244-85-2

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

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]

All Arrestin Isoforms :

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]

Chemical Information

CAS No. 1965244-85-2
Molecular Weight 523.60
Formula C₂₉H₃₄FN₃O₅
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Narayanan S, et al. Identification of potent pyrazole based APELIN receptor (APJ) agonists. Bioorg Med Chem. 2020 Feb 15;28(4):115237. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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