Chemical Name: (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
Compound Libraries
TCS OX2 29 is also offered as part of the
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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.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
10.85
25
ethanol
2.17
5
water
43.4
100
Preparing Stock Solutions
The following data is based on the product molecular weight 433.97. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.3 mL
11.52 mL
23.04 mL
5 mM
0.46 mL
2.3 mL
4.61 mL
10 mM
0.23 mL
1.15 mL
2.3 mL
50 mM
0.05 mL
0.23 mL
0.46 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Hiroseet 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
Mouldet al (2014) Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br.J.Pharmacol. 171 351 PMID: 23692283