TCS-OX2-29 (hydrochloride)

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].

Product Specifications

CAS Number

[1610882-30-8]

Product Name Alternative

OX2R antagonist

UNSPSC

12352005

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/tcs-ox2-29-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

CC(C)(C)[C@H](NCC1=CC=NC=C1)C(N2CC3=C(C=C(OC)C(OC)=C3)CC2)=O.[H]Cl

Molecular Formula

C23H32ClN3O3

Molecular Weight

433.97

References & Citations

[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.