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Submit ReviewLY 272015 hydrochloride
Description: High affinity 5-HT2B antagonist; orally active
Chemical Name: 1-[(3,4-Dimethoxyphenyl)methy]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for LY 272015 hydrochloride
LY 272015 hydrochloride is a 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
Compound Libraries for LY 272015 hydrochloride
LY 272015 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LY 272015 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LY 272015 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.29 | 100 | |
| ethanol | 3.73 | 10 |
Preparing Stock Solutions for LY 272015 hydrochloride
The following data is based on the product molecular weight 372.89. 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 | 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 for LY 272015 hydrochloride
References for LY 272015 hydrochloride
References are publications that support the biological activity of the product.
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
Niebert et al (2011) Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network. PLoS One 6 e21395 PMID: 21789169
If you know of a relevant reference for LY 272015 hydrochloride, please let us know.
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Keywords: LY 272015 hydrochloride, LY 272015 hydrochloride supplier, High, affinity, 5-HT2B, antagonists, orally, active, Serotonin, Receptors, LY272015, hydrochloride, 3077, Tocris Bioscience
3 Citations for LY 272015 hydrochloride
Citations are publications that use Tocris products. Selected citations for LY 272015 hydrochloride include:
Soll et al (2012) Expression of serotonin receptors in human hepatocellular cancer. Clin Cancer Res 18 5902 PMID: 23087410
Watts et al (2015) 5-HT is a potent relaxant in rat superior mesenteric veins. PLoS One 3 e00103 PMID: 25692021
Niebert et al (2011) Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network. J Pharmacol Exp Ther 6 e21395 PMID: 21789169
Do you know of a great paper that uses LY 272015 hydrochloride from Tocris? Please let us know.
Reviews for LY 272015 hydrochloride
Average Rating: 3 (Based on 1 Review.)
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5-HT has a potential for relaxant.
By
Anonymous on 02/18/2020
Assay Type: In Vivo
Species: Rat
LY272015 (1 lmol/L)
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.