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

Iloperidone (Synonyms: HP 873)

Cat. No.: HY-17410 Purity: 99.64%
Handling Instructions

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

For research use only. We do not sell to patients.

Iloperidone Chemical Structure

Iloperidone Chemical Structure

CAS No. : 133454-47-4

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 68 In-stock
Estimated Time of Arrival: December 31
10 mg USD 62 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 440 In-stock
Estimated Time of Arrival: December 31
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Description

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-HT1A 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-HT2A Receptor

5.6 nM (Ki)

Human 5-HT2C Receptor

42.8 nM (Ki)

In Vitro

Iloperidone displays higher affinity for the dopamine D3 receptor (Ki=7.1 nM) than for the dopamine D4 receptor (Ki=25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki=5.6 nM) than for the 5-HT2C receptor (Ki=42.8 nM)[1].

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

In Vivo

Iloperidone is eliminated slowly, with a mean t1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, tmax, or Cmax. 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].

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

Clinical Trial
Molecular Weight

426.48

Formula

C₂₄H₂₇FN₂O₄

CAS No.

133454-47-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (117.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

IloperidoneHP 873HP873HP-8735-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptoratypicalantipsychoticschizophreniasymptomsInhibitorinhibitorinhibit

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Iloperidone
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