TCS OX2 29

Cat. No. 3371

TCS OX2 29 C23H31N3O3.HCl [372523-75-6]

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Chemical Name: (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride

Biological Activity

Potent and selective OX2 receptor antagonist (IC50 = 40 nM). Displays >250-fold selectivity for OX2 over OX1 and a range of receptors, ion channels and transporters. Inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor.

Technical Data

M.Wt:
433.97
Formula:
C23H31N3O3.HCl
Solubility:
Soluble to 100 mM in water and to 25 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
372523-75-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Mould et al (2014) Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br.J.Pharmacol. 171 351. PMID: 23692283.

Hirose et al (2003) N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist. Bioorg.Med.Chem.Lett. 13 4497. PMID: 14643355.

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Citations are publications that use Tocris products. Selected citations for TCS OX2 29 include:

Plaza-Zabala et al (2013) A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior. J Mol Neurosci 38 1724. PMID: 23518606.

Urbańska et al (2012) Orexins/hypocretins acting at Gi protein-coupled OX 2 receptors inhibit cyclic AMP synthesis in the primary neuronal cultures. PLoS One 46 42561. PMID: 21547533.

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Keywords: TCS OX2 29, supplier, Potent, selective, OX2, antagonists, Orexin2, Receptors, TCSOX229, Tocris Bioscience, OX2 Receptor Antagonist products

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