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Submit ReviewTCS OX2 29
Description: Potent and selective OX2 antagonist
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 for TCS OX2 29
TCS OX2 29 is a 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 for TCS OX2 29
TCS OX2 29 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for TCS OX2 29
| M. Wt | 433.97 |
| Formula | C23H31N3O3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1610882-30-8 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TCS OX2 29
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 43.4 | 100 | |
| DMSO | 10.85 | 25 |
Preparing Stock Solutions for TCS OX2 29
The following data is based on the product molecular weight 433.97. Batch specific molecular weights may vary from batch to batch due to the degree 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 for TCS OX2 29
References for TCS OX2 29
References are publications that support the biological activity of the product.
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
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Keywords: TCS OX2 29, TCS OX2 29 supplier, Potent, selective, OX2, antagonists, Orexin2, Receptors, TCSOX229, Receptor, 3371, Tocris Bioscience
9 Citations for TCS OX2 29
Citations are publications that use Tocris products. Selected citations for TCS OX2 29 include:
Zhou et al (2015) Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats. Neuropharmacology 99 481 PMID: 26277341
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
Bian et al (2021) Orexin-B exerts excitatory effects on nigral dopaminergic neurons and alleviates motor disorders in MPTP parkinsonian mice Neurosci Lett 765 136291 PMID: 34666119
Beig et al (2015) Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus. Clin.Exp.Pharmacol.Physiol. 42 1059 PMID: 26174505
Brown et al (2013) Central orexin (hypocretin) 2 receptor antagonism reduces ethanol self-administration, but not cue-conditioned ethanol-seeking, in ethanol-preferring rats. Int.J.Neuropsychopharmacol. 16 2067 PMID: 23601187
Huang et al (2010) Orexins depolarize rostral ventrolateral medulla neurons and increase arterial pressure and heart rate in rats mainly via orexin 2 receptors. J Pharmacol Exp Ther 334 522 PMID: 20494957
Asadi (2018) The effect of intracerebroventricular administration of orexin receptor type 2 antagonist on pentylenetetrazol-induced kindled seizures and anxiety in rats. BMC Neurosci 19 49 PMID: 30103703
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
Shu et al (2014) Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals. PLoS One 9 e95259 PMID: 24748172
Do you know of a great paper that uses TCS OX2 29 from Tocris? Please let us know.
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Literature in this Area
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