Biological Activity
Potent, selective 5-HT1A receptor antagonist (IC50 = 15 nM). Selective over 5-HT1B, 1C, 2,α1, α2 and D2 receptors (IC50 > 1000 nM). Centrally active on systemic administration.
Licensing Information
Sold with the permission of Wyeth-Ayerst Research, US Patent 4,988,814
Technical Data
M. Wt | 468.47 |
Formula | C24H33N3O2.2HCl |
Storage | Desiccate at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 149007-54-5 |
PubChem ID | 6604839 |
InChI Key | NYZFUZCCDOSQBG-AWEZNQCLSA-N |
Smiles | O=C(NC(C)(C)C)[C@@]([C@]3=CC=CC=C3)([H])CN(CC2)CCN2C1=C(OC)C=CC=C1.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 | 46.85 | 100 | |
water | 2.34 | 5mM with gentle warming | |
water | 4.68 | 10mM with sonication |
Preparing Stock Solutions
The following data is based on the product molecular weight 468.47. 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 | 2.13 mL | 10.67 mL | 21.35 mL |
5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
10 mM | 0.21 mL | 1.07 mL | 2.13 mL |
50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cliffe et al (1993) (S)-N-tert-Butyl-3(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. J.Med.Chem. 36 1509 PMID: 8496920
Fletcher et al (1993) WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. Eur.J.Pharmacol. 237 283 PMID: 8365456
Fletcher et al (1993) Silent 5-HT1A receptor antagonists: utility as research tools and therapeutic agents. Trends Pharmacol.Sci. 14 41 PMID: 8122313
Rodgers and Cole (1994) Anxiolytic-like effect of (S)-WAY 100135, a 5-HT1A receptor antagonist, in the murine elevated plus-maze test. Eur.J.Pharmacol. 261 321 PMID: 7813555
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