Biological Activity
High affinity 5-HT2B receptor antagonist that displays selectivity over 5-HT2A and 5-HT2C receptors (Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors respectively). Orally active.
Licensing Information
Sold under license from Eli Lilly and company
Technical Data
| M. Wt | 372.89 |
| Formula | C21H24N2O2.HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 172895-15-7 |
| PubChem ID | 9929423 |
| InChI Key | BKAZOTIBKRWLQA-UHFFFAOYSA-N |
| Smiles | CC1=CC=C(NC3=C2CCNC3CC4=CC=C(OC)C(OC)=C4)C2=C1.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 | 37.29 | 100 | |
| ethanol | 3.73 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 372.89. 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 | 2.68 mL | 13.41 mL | 26.82 mL |
| 5 mM | 0.54 mL | 2.68 mL | 5.36 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.68 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sevoz-Couche et al (2000) In vivo modulation of vagal-identified dorsal medullary neurones by activation of different 5-Hydroxytryptamine2 receptors in rat. Br.J.Pharmacol. 131 1445 PMID: 11090119
Cohen et al (1996) LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J.Serotonin Res. 3 131 PMID:
Niebert et al (2011) Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network. PLoS One 6 e21395 PMID: 21789169
Keywords: LY 272015 hydrochloride, supplier, High, affinity, 5-HT2B, antagonists, orally, active, Serotonin, Receptors, LY272015, hydrochloride, 5-HT2B, Receptors, 5-HT2B, Receptors, Tocris Bioscience
