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Cat. No.: HY-133036

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APJ receptor agonist 1

APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC₅₀s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.

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

CAS No.: 2287153-38-0
Formula: C₃₁H₂₆ClN₃O₃
Molecular Weight:524.01

Storage:

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

Data Sheet (273 KB)

APJ receptor agonist 1 Chemical Structure

CAS No.: 2287153-38-0

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.093 nM Compound: 15a	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 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	0.12 nM Compound: 15a	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 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	0.2 nM Compound: 12f	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 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	22 nM Compound: 15b	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 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	43 nM Compound: 15b	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 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]

In Vitro

The S-atropisomer APJ receptor agonist 1 (compound 15a) is 200-fold more potent than the corresponding R-atropisomer.^[1].

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

In Vivo

APJ receptor agonist 1 (10-100 μg/min/kg; intravenous infusion) induces a 10% increase in CO with minimal impact on blood pressure (<5% transient blood pressure drop)^[1].

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

Animal Model:

Isoflurane-anesthetized male Sprague Dawley rats^[1]
Dosage:

10, 100, 1000 μg/kg/min
Administration:

IV; infused into the jugular vein for 15 min
Result:

Showed a dose-dependent improvement in the cardiac output in male Sprague Dawley rats with no significant changes in either mean arterial blood pressure or heart rate.

Chemical Information

CAS No. 2287153-38-0
Molecular Weight 524.01
Formula C₃₁H₂₆ClN₃O₃
SMILES

O=C(C1=CC(C(N[C@@H](C2=CC=CC=C2)CCC)=O)=CC=[C@]1[C@]3=C(Cl)C=CC=C3C4=NC5=CC=CC=C5N4)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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Su S, Clarke A, et al. Biphenyl Acid Derivatives as APJ Receptor Agonists. J Med Chem. 2019;62(22):10456-10465. [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.

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100 mg

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