TCS OX2 29

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Cat.No. 3371 - TCS OX2 29 | C23H31N3O3.HCl | CAS No. 1610882-30-8
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 (8)
Reviews
Literature (3)

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 2.0 Max. 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 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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 43.4 100
DMSO 10.85 25

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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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

8 Citations for TCS OX2 29

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

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

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

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


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