LY 272015 hydrochloride

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Cat.No. 3077 - LY 272015 hydrochloride | C21H24N2O2.HCl | CAS No. 172895-15-7
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)
Datasheet
Citations (3)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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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

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

Watts et al (2015) 5-HT is a potent relaxant in rat superior mesenteric veins. PLoS One 3 e00103 PMID: 25692021


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5-HT Receptors

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.

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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.

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