372523-75-6

372523-75-6 structure

Name: TCS-OX2-29
Chemical Name: TCS OX2 29
CAS Number: 372523-75-6
Molecular Formula: C₂₃H₃₁N₃O₃
Molecular Weight: 397.51
Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
Create Date: 2018-06-20 20:04:02
Modify Date: 2024-01-10 13:25:20
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]

Name	TCS OX2 29
Synonyms	8-Bromo-cGMP,sodium salt (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanonehydrochloride TCS-OX2-29

Description	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]
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor) Research Areas >> Cancer
References	[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.