JNJ-63533054

• CAT Number: I002346
• CAS Number: 1802326-66-4
• Molecular Formula: C17H17ClN2O2
• Molecular Weight: 316.78
• Purity: ≥95%
• Target: hGPR139
• Solubility: 10 mM in DMSO
• Storage: room temp
• IC50: 16 nM (EC50)
• IUPAC Name: 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide
• InChI: InChI=1S/C17H17ClN2O2/c1-12(13-6-3-2-4-7-13)20-16(21)11-19-17(22)14-8-5-9-15(18)10-14/h2-10,12H,11H2,1H3,(H,19,22)(H,20,21)/t12-/m0/s1
• InChIKey: MWDVCHRYCKXEBY-LBPRGKRZSA-N
• SMILES: C[C@@H](C1=CC=CC=C1)NC(=O)CNC(=O)C2=CC(=CC=C2)Cl

JNJ 63533054（Cat No.:I002346） is a powerful and specific agonist of GPR139, a receptor in the human body. It demonstrates potent activation of human GPR139 in calcium mobilization and GTPγS binding assays, with EC50 values of 16 ± 6 nM and 17 ± 4 nM, respectively. This suggests that JNJ 63533054 has a strong affinity for GPR139 and effectively triggers its activity. Understanding the activation and modulation of GPR139 can provide insights into its potential role in various physiological and pathological processes, making JNJ 63533054 a valuable tool for further research in this area.

Reference

[1]. Dvorak CA, et al. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.

[2]. Liu C, et al. GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine. Mol Pharmacol. 2015 Nov;88(5):911-25.