AZD5462

SKU: orb1686198

Description

AZD5462 is a potent and orally bioavailable small molecule agonist of the relaxin receptor RXFP1. It is utilized in preclinical research to investigate therapeutic pathways for heart failure and cancer, supporting both in vitro mechanistic studies and in vivo disease models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2787501-83-9
• MW: 544.65
• Purity: 99.63% (May vary between batches)
• Formula: C₃₀H₄₁FN₂O₆
• SMILES: C(NCC1(C)CCC1)(=O)[C@@H]2[C@H](NC(=O)C3=C(OC)C=C(F)C(O[C@H]4CC[C@](C(O)=O)(C)CC4)=C3)[C@@]5(C[C@]2(CC5)[H])[H]
• Target: RXFP receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.67 mM);DMSO:150 mg/mL (275.41 mM)

Bioactivity

• Target IC50:
  cGMP:50 nM (EC50s)|cAMP:17 nM (EC50s)
• In Vitro:
  AZD5462 (example 1) exhibits stimulatory activity on cAMP or cGMP production with EC50s of 17 nM and 50 nM, respectively. Binding to human plasma proteins with a fraction unbound (free) rate of 4.3%, AZD5462 demonstrates stability with Clint values of 23 μL/min/mg (human liver microsomal), 4.8 μL/min/10^6 cells (human hepatocyte), and 11 μL/min/10^6 cells (rat hepatocyte). AZD5462 enhances the phosphorylation of ERK with an EC50 value of 6.3 nM.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RXFPreceptor, RXFP receptor, RXFP1

Compound Identifiers

PubChem CID

163395232