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 Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 433.97 |
| Formula | C23H31N3O3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 372523-75-6 |
| PubChem ID | 53302033 |
| InChI Key | NHKNHFJTMINMBP-ZMBIFBSDSA-N |
| Smiles | C[C@@](C)(C)[C@H](NCC3=CC=NC=C3)C(N(C2)CCC1=C2C=C(OC)C(OC)=C1)=O.Cl |
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 |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Mould et al (2014) Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br.J.Pharmacol. 171 351 PMID: 23692283
Keywords: TCS OX2 29, supplier, Potent, selective, OX2, antagonists, Orexin2, Receptors, TCSOX229, OX2, Receptor, OX2, Receptor, Tocris Bioscience
