Art. -Nr.: HY-17410

Iloperidone

(Synonyms: HP 873)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Iloperidone (HP 873) is a D₂/5-HT₂ receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.

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Reinheit: 99.93%
CAS. Nr.: 133454-47-4
Formel: C₂₄H₂₇FN₂O₄
Molecular Weight:426.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Iloperidone Chemical Structure

CAS. Nr.: 133454-47-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Iloperidone (HP 873) is a D₂/5-HT₂ receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms^[1]^[2].

IC₅₀ & Target^[1]

Rat D₂ Receptor

54 nM (Ki)

Rat 5-HT₂ Receptor

3.1 nM (Ki)

Rat D₁ Receptor

546 nM (Ki)

Rat 5-HT_1A Receptor

168 nM (Ki)

Rat 5-HT₆ Receptor

42.7 μM (Ki)

Rat 5-HT₇ Receptor

21.6 nM (Ki)

Human D₁ Receptor

216 nM (Ki)

Human D₃ Receptor

7.1 nM (Ki)

Human D₄ Receptor

25 nM (Ki)

Human D₅ Receptor

319 nM (Ki)

Human 5-HT_2A Receptor

5.6 nM (Ki)

Human 5-HT_2C Receptor

42.8 nM (Ki)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Iloperidone displays higher affinity for the dopamine D₃ receptor (K_i=7.1 nM) than for the dopamine D₄ receptor (K_i=25 nM). Iloperidone displays high affinity for the 5-HT₆ and 5-HT₇ receptors (K_i=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT_2A (Ki=5.6 nM) than for the 5-HT_2C receptor (K_i=42.8 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Iloperidone is eliminated slowly, with a mean t_1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, t_max, or C_max. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 133454-47-4
Appearance Solid
Molecular Weight 426.48
Formel C₂₄H₂₇FN₂O₄
Color White to off-white
SMILES

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

HP 873
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Drug Metab Dispos

2025 Dec 22.
Neuroreport

Effects of iloperidone on hERG 1A/3.1 heterotetrameric channels. [Abstract]

2021 Nov 2;32(16):1299-1306. PMID: 34605450

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (117.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

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

[2]. Sainati, S.M., et al., 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. [Content Brief]

[3]. Albers, L.J., A. Musenga, and M.A. Raggi, 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3448 mL	11.7239 mL	23.4478 mL	58.6194 mL
	5 mM	0.4690 mL	2.3448 mL	4.6896 mL	11.7239 mL
	10 mM	0.2345 mL	1.1724 mL	2.3448 mL	5.8619 mL
	15 mM	0.1563 mL	0.7816 mL	1.5632 mL	3.9080 mL
	20 mM	0.1172 mL	0.5862 mL	1.1724 mL	2.9310 mL
	25 mM	0.0938 mL	0.4690 mL	0.9379 mL	2.3448 mL
	30 mM	0.0782 mL	0.3908 mL	0.7816 mL	1.9540 mL
	40 mM	0.0586 mL	0.2931 mL	0.5862 mL	1.4655 mL
	50 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL
	60 mM	0.0391 mL	0.1954 mL	0.3908 mL	0.9770 mL
	80 mM	0.0293 mL	0.1465 mL	0.2931 mL	0.7327 mL
	100 mM	0.0234 mL	0.1172 mL	0.2345 mL	0.5862 mL

Keywords

Iloperidone

2 Cited Publications

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Iloperidone

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Publications Citing Use of MedChemExpress (MCE) Iloperidone

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Iloperidone Related Classifications

Art. -Nr.: HY-17410