1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Lorcaserin Hydrochloride (Synonyms: APD356)

Cat. No.: HY-15368 Purity: 99.94% ee.: 100.00%
Handling Instructions

Lorcaserin (Hydrochloride) is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.

For research use only. We do not sell to patients.
Lorcaserin Hydrochloride Chemical Structure

Lorcaserin Hydrochloride Chemical Structure

CAS No. : 846589-98-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
5 mg USD 60 In-stock
10 mg USD 84 In-stock
50 mg USD 168 In-stock
100 mg USD 252 In-stock
200 mg USD 372 In-stock
500 mg USD 540 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


Lorcaserin (Hydrochloride) is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.

IC50 & Target

Ki: 15 nM (5-HT2C)

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)[1].

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[2].

Clinical Trial
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 4.3076 mL 21.5378 mL 43.0756 mL
5 mM 0.8615 mL 4.3076 mL 8.6151 mL
10 mM 0.4308 mL 2.1538 mL 4.3076 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay

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. In brief, 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Lorcaserin is formulated in deionized water.

Male Sprague-Dawley rats (250-300 g) are obtained from Harlan. 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. Lorcaserin is formulated in deionized water. The following sampling scheme is used (n=3/time point): 0.25, 0.5, 1, 2, 4, 8, 12, 24, and 40 h after dose. Rats are lightly anesthetized with isoflurane, blood is collected via cardiac puncture, and brains are removed from the cranium. Blood samples are dispensed into sodium-heparinized vials, and then vials are capped and stored at 4°C. Plasma is separated from formed elements in blood by centrifugation (10 min at 3000 g), and then plasma is frozen. Brains are rinsed with ice-cold phosphate-buffered saline, blotted dry, weighed, and frozen. Plasma and brain samples are stored at -80°C before bioanalytical analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight







ClC1=CC=C2C([[email protected]@H](C)CNCC2)=C1.[H]Cl

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 2.4 mg/mL

Lorcaserin hydrochloride is dissolved in sterile 0.9% saline[3].

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


Purity: 99.94% ee.: 100.00%

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