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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
OX2 Receptor
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