Iloperidone (HP-873)

Alias: HP873; Iloperidone, Fanapt; HP-873; HP 873; iloperidone; Zomaril

Cat No.:V1037 Purity: ≥98%

COA Product Data Instructions for use SDS

Iloperidone (Fanapt, HP-873; HP 873; Zomaril), an atypical antipsychotic agent, is a potent antagonist of dopamine (D2)/serotonin (5-HT2) receptor which has been approved for the treatment of schizophrenia symptoms.

Iloperidone (HP-873) Chemical Structure CAS No.: 133454-47-4
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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Top Publications Citing lnvivochem Products

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

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Cancer Cell 2021,39(4):529-547.e7.

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Immunity 2023,56(3):620-634.e11.

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.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

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

Biological Activity I Assay Protocols (From Reference)

Targets

Rat D₂ Receptor ( Ki = 54 nM ); Rat 5-HT₂ Receptor ( Ki = 3.1 nM ); Rat D₁ Receptor ( Ki = 546 nM );
Rat 5-HT_1A Receptor ( Ki = 168 nM ); Rat 5-HT₆ Receptor ( Ki = 42.7 nM ); Rat 5-HT₇ Receptor ( Ki = 21.6 nM );
Human D₁ Receptor ( Ki = 216 nM ); Human D₃ Receptor ( Ki = 7.1 nM ); Human D₄ Receptor ( Ki = 25 nM );
Human D₅ Receptor ( Ki = 319 nM ); Human 5-HT_2A Receptor ( Ki = 5.6 nM ); Human 5-HT_2C Receptor ( Ki = 42.8 nM )

ln Vitro

In vitro activity: Iloperidone exhibits greater affinity (K_i=7.1 nM) for the dopamine D₃ receptor as compared to the dopamine D₄ receptor (K_i=25 nM). Iloperidone is found to have a higher affinity for the 5-HT_2A receptor (K_i=5.6 nM) than for the 5-HT_2C receptor (K_i=42.8 nM), and it exhibits high affinity for both the 5-HT₆ and 5-HT₇ receptors (K_i=42.7 and 21.6 nM, respectively)[1].

ln Vivo

Iloperidone has a mean half-life of 13.5 to 14.0 hours, indicating a slow elimination rate. AUC, t_max, and C_max were not significantly impacted by coadministration with food. These findings suggest that taK_ing iloperidone with food slows down the drug's absorption rate while maintaining the same level of overall bioavailability. The most frequently reported adverse events were somnolence, dizziness, and orthostatic hypotension[2].

Enzyme Assay

Iloperidone (HP 873) is an atypical antipsychotic that works as a D2/5-HT2 receptor antagonist to treat symptoms of schizophrenia. Compared to the dopamine D4 receptor (Ki = 25 nM), iloperidone exhibited a greater affinity for the dopamine D3 receptor (Ki = 7.1 nM). Iloperidone was found to have a higher affinity for the 5-HT2A receptor (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM), and to have a high affinity for both the 5-HT6 and 5-HT7 receptors (Ki = 42.7 and 21.6 nM, respectively).

Animal Protocol

1, 3, 10 mg/kg

N/A

References

[1]. Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol, 1996. 317(2-3): p. 417-23.

[2]. Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol, 1995. 35(7): p. 713-20.

[3]. Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? Expert Opin Investig Drugs, 2008. 17(1): p. 61-75.

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

Physicochemical Properties

Molecular Formula

C24H27FN2O4

Molecular Weight

426.48

Exact Mass

426.2

Elemental Analysis

C, 67.59; H, 6.38; F, 4.45; N, 6.57; O, 15.01

CAS #

133454-47-4

Related CAS #

Iloperidone metabolite Hydroxy Iloperidone; 133454-55-4; Iloperidone hydrochloride; 1299470-39-5; Iloperidone-d3; 1071167-49-1

Appearance

Solid powder

SMILES

CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC

InChi Key

XMXHEBAFVSFQEX-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H27FN2O4/c1-16(28)18-4-7-21(23(14-18)29-2)30-13-3-10-27-11-8-17(9-12-27)24-20-6-5-19(25)15-22(20)31-26-24/h4-7,14-15,17H,3,8-13H2,1-2H3

Chemical Name

1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-methoxyphenyl]ethanone

Synonyms

HP873; Iloperidone, Fanapt; HP-873; HP 873; iloperidone; Zomaril

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: 27~50 mg/mL (63.3~117.2 mM)

Water: <1 mg/mL

Ethanol: ~4 mg/mL (~9.4 mM)

Solubility (In Vivo)

2%DMSO+40%PEG 300+dd H2O: 2mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3448 mL	11.7239 mL	23.4478 mL
	5 mM	0.4690 mL	2.3448 mL	4.6896 mL
	10 mM	0.2345 mL	1.1724 mL	2.3448 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*

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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)

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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

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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

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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

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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
NCT04819776	Active Recruiting	Drug: Iloperidone Drug: Iloperidone Placebo	Bipolar I Disorder	Vanda Pharmaceuticals	March 22, 2021	Phase 3
NCT05344365	Recruiting	Drug: Iloperidone	Parkinson Disease Psychosis	Vanda Pharmaceuticals	June 2022	Phase 2
NCT05648591	Recruiting	Drug: Iloperidone	Schizophrenia Bipolar I Disorder	Vanda Pharmaceuticals	May 24, 2023	Phase 4
NCT02413918	Completed	Drug: iloperidone	Bipolar Disorder	The University of Texas Health Science Center at San Antonio	April 2012	Phase 4
NCT04712734	Completed	Drug: Iloperidone	Schizophrenia	Vanda Pharmaceuticals	January 13, 2021	Phase 1

Biological Data

Bargraph of selected receptor affinities (pKI in nM) of iloperidone.Neuropsychopharmacology.2001 Dec;25(6):904-14.