TCS-OX2-29

TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.target: OX2 IC 50: 40 nMIn vitro:TCS-OX2-29 shows selectivity for ion channels, and transporters (<30% inhibition at 10 μM), which includes G-protein coupled receptors associated with food intake including galanin and neuripeptide Y. [1]TCS-OX2-29 Inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor. [2]

Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)

Research Areas >> Cancer

[1]. Hirose M et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidicantagonist. Bioorg Med Chem Lett, 2003 Dec 15, 13(24):4497-9.

[2]. R Mould et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan; 171(2): 351-363.

SB 334867 | lemborexant | Almorexant HCI | Filorexant | Orexin 2 Receptor Agonist | MK-1064 | SB-674042 | GSK1059865 | IPSU | SB408124 | MK-3697 | Nemorexant | Orexin B (mouse, rat) | SB-649868 | TCS 1102