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Submit ReviewRO 5263397 hydrochloride is a potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice.
RO 5263397 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 230.67 |
Formula | C10H11FN2O.HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
InChI Key | JFAYMXKBMDRFHY-SBSPUUFOSA-N |
Smiles | CC1=C([C@H]2COC(N)=N2)C=CC=C1F.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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 23.07 | 100 | |
water | 23.07 | 100 |
The following data is based on the product molecular weight 230.67. 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 | 4.34 mL | 21.68 mL | 43.35 mL |
5 mM | 0.87 mL | 4.34 mL | 8.67 mL |
10 mM | 0.43 mL | 2.17 mL | 4.34 mL |
50 mM | 0.09 mL | 0.43 mL | 0.87 mL |
References are publications that support the biological activity of the product.
Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID: 29977204
Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID: 26985297
Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID: 27658486
If you know of a relevant reference for RO 5263397 hydrochloride, please let us know.
Keywords: RO 5263397 hydrochloride, RO 5263397 hydrochloride supplier, Trace, amine, associated, receptor, 1, agonists, agonism, TAR, TA1, TAAR1, locomotion, waking, REM, NREM, sleep, Amine, Receptor, 6833, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.