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

Iloperidone (Synonyms: HP 873)

Cat. No.: HY-17410 Purity: 99.93%
Handling Instructions

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

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

Iloperidone Chemical Structure

Iloperidone Chemical Structure

CAS No. : 133454-47-4

Size Price Stock Quantity
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
200 mg   Get quote  
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Description

Iloperidone(HP 873) is a D2/5-HT2 receptor antagonist, which is an atypical antipsychotic for the treatment of schizophrenia symptoms. IC50 value: Target: 5-HT receptor; D2 receptor Iloperidone (HP 873) is a compound currently in clinical trials for the treatment of schizophrenia. Iloperidone displays affinity for dopamine D2 receptors and for 5-HT2A receptors and has a variety of in vivo activities suggestive of an atypical antipsychotic. Iloperidone displayed higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displayed high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 and 21.6 nM, respectively), and was found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM) [1]. Iloperidone was 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]. Iloperidone pharmacokinetics and pharmacodynamics are presented herein, together with an evaluation of clinical safety and efficacy results [3]. Clinical indications: Post traumatic stress disorder; Schizophrenia Toxicity: Commonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased.

Clinical Trial
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
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

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Product Name:
Iloperidone
Cat. No.:
HY-17410
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Iloperidone

Cat. No.: HY-17410