1610882-30-8

1610882-30-8 structure

Name: TCS OX2 29
Chemical Name: (2S)-1-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride (1:1)
CAS Number: 1610882-30-8
Molecular Formula: C₂₃H₃₂ClN₃O₃
Molecular Weight: 433.971
Create Date: 2018-06-25 00:22:14
Modify Date: 2024-01-09 16:22:00
TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[1][2].

Name	(2S)-1-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride (1:1)
Synonyms	(2S)-1-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride (1:1) (2S)-1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3,3-dimethyl-2-[(pyridin-4-ylmethyl)amino]butan-1-one hydrochloride (1:1) 1-Butanone, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-, (2S)-, hydrochloride (1:1)

Description	TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[1][2].
Related Catalog	Research Areas >> Cancer Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)
References	[1]. Hirose M, et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4497-9. [2]. Tabaeizadeh M, et al. The differential effects of OX1R and OX2R selective antagonists on morphine conditioned place preference in naïve versus morphine-dependent mice. Behav Brain Res. 2013 Jan 15;237:41-8. [3]. Mould R, et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan;171(2):351-63.