APJ receptor agonist 4
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
For research use only. We do not sell to patients.
- CAS No.: 2762567-70-2
- Formula: C28H28ClFN6O3
- Molecular Weight:551.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
apelin receptor[1]
| species | rat | monkey | dogmax (ng/mL) |
| dose (mg/kg) | 1 (i.v. and p.o.) | 1 (i.v.) and 3 (p.o.) | 1 (i.v. and p.o.) |
| vehiclea | F | G | G |
| CI (mL/min/kg) | 4.6 | 10.6 | 2.4 |
| VSS (L/kg) | 1.6 | 0.2 | 0.2 |
| T1/2 (h) | 4.0 | 1.3 | 2.5 |
| Cmax (μM•h) | 2.2 | 1.4 | 6.5 |
| AUC0-24 (μM•h) | 3.7 | 2.5 | 14.2 |
| F (%) | 54 | 27 | 76 |
a: Vehicle F: 5/5/90 v/v/v DMAC/Cremophor EL/sodium carbonate buffer, pH 9 and vehicle G: 10/40/50 v/v/v ethanol/PEG400/sodium carbonate buffer, pH 9.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2762567-70-2
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Molecular Weight 551.01
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Formula C28H28ClFN6O3
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SMILES
O=C1C(C(N2CC[C@@H](C3=C(F)C=C(Cl)C=N3)C2)=O)=C(O)N(C4=C(CC)C=CC=C4CC)C(C5=NN(C)C=C5)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
APJ receptor agonist 4 Related Classifications
HY-145284 Related Classifications
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