Biological Activity
Selective and high affinity 5-HT6 antagonist (pKi = 8.9); displays low hERG inhibition. Exhibits >100 fold selectivity against a panel of 50 targets including other 5-HT receptor subtypes. Brain penetrant.
Compound Libraries
R 1485 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 450.35 |
Formula | C18H20FN3O3S.2HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
PubChem ID | 90488993 |
InChI Key | SNXURKRGPYXWRN-UHFFFAOYSA-N |
Smiles | FC(C=CC=C4)=C4S(N2CCOC1=C(N3CCNCC3)C=CC=C12)(=O)=O.Cl.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 | 45.03 | 100 | |
water | 45.03 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 450.35. 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 | 2.22 mL | 11.1 mL | 22.2 mL |
5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zhao et al (2007) 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists. Bioorg.Med.Chem.Lett. 17 3504 PMID: 17485206
Liu et al (2009) 5-HT6 antagonists as potential treatment for cognitive dysfunction. Drug Des.Rev. 70 145 PMID:
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