JNJ-63533054

SKU: orb1304517

Description

JNJ-63533054 is a selective and potent agonist for the human GPR139 receptor, exhibiting an EC50 of 16 nM. This research compound is a valuable tool for investigating GPR139 function in both in vitro assays and in vivo models related to neurological and metabolic research.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1802326-66-4
• MW: 316.78
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₁₇ClN₂O₂
• SMILES: C[C@H](NC(=O)CNC(=O)c1cccc(Cl)c1)c1ccccc1
• Target: GPCR
• Solubility: DMSO:45 mg/mL (142.05 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.31 mM)

Bioactivity

• Target IC50:
  GPR139:16 Nm(EC50)
• In Vivo:
  JNJ-63533054 is found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat. JNJ-63533054 exhibits good stability in both human and rat microsomes and high solubility in aqueous media, and no DDI potential was found. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM).
• In Vitro:
  JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. JNJ-63533054 is found to be clean of any cross reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters as well as our own internal whole cell lead generation biology selectivity panel.

Storage & Handling

• Storage: 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

oral, JNJ63533054, JNJ-63533054, JNJ 63533054, inhibit, L-phenylalanine, L-tryptophan, hGPR139, Inhibitor, G Protein-Coupled Receptor 139, GPR139, barrier, blood-brain, CNS

Compound Identifiers

PubChem CID

2548547