Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
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.
Targets |
Rat D2 Receptor ( Ki = 54 nM ); Rat 5-HT2 Receptor ( Ki = 3.1 nM ); Rat D1 Receptor ( Ki = 546 nM );
Rat 5-HT1A 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-HT2A Receptor ( Ki = 5.6 nM ); Human 5-HT2C Receptor ( Ki = 42.8 nM ) |
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ln Vitro |
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ln Vivo |
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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).
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Animal Protocol |
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References |
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Molecular Formula |
C24H27FN2O4
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Molecular Weight |
426.48
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Exact Mass |
426.2
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Elemental Analysis |
C, 67.59; H, 6.38; F, 4.45; N, 6.57; O, 15.01
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CAS # |
133454-47-4
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Related CAS # |
Iloperidone metabolite Hydroxy Iloperidone; 133454-55-4; Iloperidone hydrochloride; 1299470-39-5; Iloperidone-d3; 1071167-49-1
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Appearance |
Solid powder
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SMILES |
CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC
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InChi Key |
XMXHEBAFVSFQEX-UHFFFAOYSA-N
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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
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Chemical Name |
1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-methoxyphenyl]ethanone
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
(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.
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 |