TCS OX2 29

Pricing Availability Delivery Time Qty
Cat.No. 3371 - TCS OX2 29 | C23H31N3O3.HCl | CAS No. 372523-75-6
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)
Datasheet
Citations (7)
Reviews
Literature

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

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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
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
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Safety Datasheet

References

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

7 Citations for TCS OX2 29

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

Zhou et al (2015) Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats. Neuropharmacology 99 481 PMID: 26277341

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

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

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


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