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Lorcaserin HCl

Catalog No. T6572   CAS 846589-98-8

Lorcaserin is a selective serotonin agonist that has been recently approved as a weight loss agent.

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Lorcaserin HCl Chemical Structure
Lorcaserin HCl, CAS 846589-98-8
Pack Size Availability Price/USD Quantity
5 mg In stock $ 50.00
10 mg In stock $ 70.00
25 mg In stock $ 114.00
50 mg In stock $ 167.00
100 mg In stock $ 248.00
500 mg In stock $ 535.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.86%
Purity: 99.16%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lorcaserin is a selective serotonin agonist that has been recently approved as a weight loss agent.
In vitro Lorcaserin is 18-fold more potent at human 5-HT2C (EC50= 9 nM) than at human 5-HT2A (EC50= 168 nM), and it is 104-fold more potent at human 5-HT2C than human 5-HT2B (EC50= 943 nM)
In vivo Lorcaserin decreases cumulative food intake at 2, 4, 6, and 22 h with a significant decrease continuing throughout the 22-h duration of the study at the highest dose (24 mg/kg) only. The reduction in food intake induced by lorcaserin (18 mg/kg, p.o.) is mediated by 5-HT2C and not 5-HT2A receptors. Lorcaserin significantly reduces active, and increased inactive counts, and increases the incidence of penile grooming, an effect mediated by the 5-HT2C receptor[1]. Lorcaserin (20 mg/kg) doses causes a significant linear dose-related reduction in responses on the active lever but has no significant effect on the response to the inactive lever. Lorcaserin (0.3125, 0.625, 1.25, and 2.5 mg/kg) also produces a significant reduction in nicotine self-administration[
Cell Research For development of functional human and rat 5-HT2A,5-HT2B,and 5-HT2C inositol accumulation assays,recombinant 5-HT2 receptors are transiently expressed in HEK293 cells using the Lipofectamine method.Cells are incubated in 15-cm plates with DMEM,and they are grown to at least 60 to 80% confluence,rinsed with Opti-MEM I media,followed by addition of 2 mL of Opti-MEM I containing 60 μL of Lipofectamine and 16 μg of cDNA for human and rat 5-HT2A and 5-HT2B receptors or 15 μL of Lipofectamine and 16 μg of cDNA for human and rat 5-HT2C receptors.Cells are then incubated for 5 h at 37°C in a 5% CO2 incubator.Next,cells are aspirated,and 30 mL of DMEM is added.Cells are then used for assays 24 h after transfection.Under these conditions,cells expressing human 5-HT2C receptor display constitutive elevation of inositol phosphate accumulation that is reversed by the inverse agonist mianserin,whereas cells expressing human 5-HT2A and 5-HT2B receptors display considerably less constitutive activity.
Animal Research On the day of the experiment, rats receives a single dose of lorcaserin in water via oral gavage. Dosing volume and dose are 5 mL/kg and 10 mg/kg, respectively.
Molecular Weight 232.15
Formula C11H14ClN·HCl
CAS No. 846589-98-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 2.4 mg/mL (10.34 mM)

Ethanol: 46 mg/mL (198.14 mM)

H2O: 46 mg/mL (198.14 mM)

TargetMolReferences and Literature

1. Thomsen WJ, et al. J Pharmacol Exp Ther, 2008, 325(2), 577-587. 2. Levin ED, et al. J Pharmacol Exp Ther, 2011, 338(3), 890-896.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library ReFRAME Related Library Neurotransmitter Receptor Compound Library Serotonin Receptor-Targeted Compound Library Anti-Cancer Compound Library

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Keywords

Lorcaserin HCl 846589-98-8 GPCR/G Protein Neuroscience 5-HT Receptor inhibitor inhibit

 

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