1. GPCR/G Protein
  2. Apelin Receptor (APJ) Arrestin
  3. B-007

B-007 is an AplnR agonist with G protein-biased signaling (EC50 = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure.

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

B-007

B-007 Chemical Structure

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Description

B-007 is an AplnR agonist with G protein-biased signaling (EC50 = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure[1].

IC50 & Target[1]

Arrestin-2/β-Arrestin 1

 

Arrestin-3/β-Arrestin 2

 

In Vitro

B-007 potently activates the AplnR G protein pathway in cell systems expressing the Apelin receptor (AplnR), with an EC50 of 11.6 nM and an Emax of 118.0%[1].
B-007 completely fails to activate the β-arrestin1 or β-arrestin2 pathways of the AplnR in AplnR-expressing cell systems, thereby exhibiting prominent G protein-biased characteristics[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

717.62

Formula

C32H24F5N5O7S

SMILES

COC1=CC=CC(OC)=C1C2=NC(C(NS(C(C3=CC=CC=C3)COC(C4=C(F)C(F)=C(F)C(F)=C4F)=O)(=O)=O)=O)=NN2C5=CN=CC(C)=C5

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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    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:
B-007
Cat. No.:
HY-183777
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