Lorcaserin HCl

Alias: APD 356; Lorcaserin hydrochloride; Belviq Xr; Lorcaserin HCl; APD-356; APD356; Lorqess

Cat No.:V1032 Purity: ≥98%

COA Product Data Instructions for use SDS

Lorcaserin HCl Chemical Structure CAS No.: 846589-98-8
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

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Nature 2024 Dec 18.

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Nature 597, 119–125 (2021)

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Lorcaserin HCl (Belviq Xr; APD-356; APD356; Lorqess), the hydrochloride salt of Lorcaserin which is a marketed weight-loss drug, is a potent and selective full agonist of human 5-HT2C (serotonin) receptor with Ki of 15 nM. It suppresses appetite by triggering the hypothalamic 5-HT_2C receptor, which is known to regulate appetite.

Biological Activity I Assay Protocols (From Reference)

Targets

RAAS

ln Vitro

In vitro activity: Lorcaserin shows greater affinity for human 5-HT2C compared to 5-HT 5-HT2A (7.5-fold selective, Ki=112 nM) and 5-HT 5-HT2B (11.6-fold selective, Ki=174 nM). All three of the human 5-HT2 receptors are active when lorcaserin is present. Lorcaserin is 104 times more potent at human 5-HT2C than at human 5-HT2B (EC50= 943 nM), and it is 18 times more potent at human 5-HT2C (EC50= 9 nM) than at human 5-HT2A (EC50= 168 nM). Human 5-HT2C and 5-HT2B receptors exhibit full agonist activity, while human 5-HT2A receptors exhibit partial agonist activity (100%, 100%, and 75% of the maximal response elicited by serotonin, respectively). When it comes to ligand binding to serotonin, dopamine, and norepinephrine transporters, lorcaserin is not a rival. In rat synaptosomes, lorcaserin does not increase the release of norepinephrine, dopamine, or serotonin at submicromolar concentrations. Lorcaserin weakly blocks the uptake of dopamine (EC50= 12,000 nM), serotonin (EC50= 1400 nM), and norepinephrine (EC50= 2500 nM).

ln Vivo

Lorcaserin produces reduces food intake and body weight gain during the 4-week trial in a dose-dependent manner. Lorcaserin (18 mg/kg) has no effect on rats' back muscle contractions or wet dog shakes, but it dramatically increases penile grooming and resting. In female rats, nicotine self-administration is significantly reduced by lorcaserin short-term administration (0.3125–20 mg/kg). Over the course of two weeks of repeated injections, long-term lorcaserin (0.625 mg/kg) also significantly lowers nicotine self-administration.

Animal Protocol

0.3125-20 mg/kg; injections

Rats

References

[1]. J Pharmacol Exp Ther . 2008 May;325(2):577-87.

[2]. J Pharmacol Exp Ther . 2011 Sep;338(3):890-6.

Additional Infomation

Lorcaserin hydrochloride is a hydrochloride obtained by reaction of lorcaserin with one equivalent of hydrochloric acid. Used as an anti-obesity drug. It has a role as a serotonergic agonist and an appetite depressant. It contains a lorcaserin(1+).
See also: Lorcaserin (has active moiety); Lorcaserin hydrochloride hemihydrate (annotation moved to).

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C11H15CL2N

Molecular Weight

232.15

Exact Mass

231.058

CAS #

846589-98-8

Related CAS #

846589-98-8(HCl)

PubChem CID

11673085

Appearance

Typically exists as solid at room temperature

LogP

3.72

Hydrogen Bond Donor Count

Hydrogen Bond Acceptor Count

Rotatable Bond Count

Heavy Atom Count

Complexity

172

Defined Atom Stereocenter Count

SMILES

C[C@H]1CNCCC2C=CC(=CC1=2)Cl.Cl

InChi Key

ITIHHRMYZPNGRC-QRPNPIFTSA-N

InChi Code

InChI=1S/C11H14ClN.ClH/c1-8-7-13-5-4-9-2-3-10(12)6-11(8)9;/h2-3,6,8,13H,4-5,7H2,1H3;1H/t8-;/m0./s1

Chemical Name

(5R)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine;hydrochloride

Synonyms

APD 356; Lorcaserin hydrochloride; Belviq Xr; Lorcaserin HCl; APD-356; APD356; Lorqess

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 46~100 mg/mL (198.1~109.2 mM)

Water: ~46 mg/mL (~198.1 mM)

Ethanol: ~46 mg/mL (~198.1 mM)

Solubility (In Vivo)

5%DMSO + 40%PEG300 + 5%Tween 80: 5.0mg/ml (5.46mM) (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02400359	Active Recruiting	Drug: Lorcaserin HCl Drug: Placebo	Obesity Weight Loss	Beth Israel Deaconess Medical Center	October 2014	Phase 4
NCT02019264	Completed	Drug: Lorcaserin hydrochloride Drug: Placebo	Obesity Overweight Type 2 Diabetes	Eisai Inc.	January 24, 2014	Phase 4
NCT02398669	Completed	Drug: Lorcaserin hydrochloride	Obesity	Eisai Inc.	March 2015	Phase 1
NCT00829140	Completed	Drug: Placebo Drug: Lorcaserin 10mg BID	Obesity	Eisai Inc.	November 2008	Phase 1
NCT00395135	Completed	Drug: Lorcaserin 10 mg BID Drug: Matching Placebo BID	Obesity	Eisai Inc.	November 2006	Phase 3

Biological Data

A, short-term dose-effect function of the higher dose range of lorcaserin on nicotine-self-administration (mean ± S.E.M.).J Pharmacol Exp Ther.2011 Sep;338(3):890-6.
A, short-term dose-effect function of the lower dose range of lorcaserin on nicotine-self-administration (mean ± S.E.M.).J Pharmacol Exp Ther.2011 Sep;338(3):890-6.
A, chronic lorcaserin administration effect on locomotor activity over 2 weeks of treatment averaged over 12 5-min blocks.J Pharmacol Exp Ther.2011 Sep;338(3):890-6.