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133454-47-4 (Iloperidone)

1

Identification

Iloperidone Iloperidone
Name Iloperidone
Formula C24H27FN2O4
MW 426.48
CAS No. 133454-47-4
EINECS
Smiles FC1=CC2=C(C=C1)C(C3CCN(CCCOC4=C(OC)C=C(C(C)=O)C=C4)CC3)=NO2
Synonyms 1-[4-[3-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]ethanone; 1-(4-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propoxy)-3-methoxyphenyl)ethanone
InChI 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
2

Introduction

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.

Background Information

D2/5-HT2 antagonist as an antipsychotic agent ......by AOBIOUS INC
Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. ......by AbMole BioScience
Iloperidone is an atypical antipsychotic for the treatment of schizophrenia. ......by AdooQ BioScience, LLC
Iloperidone is an atypical antipsychotic for the treatment of schizophrenia symptoms. ......by MedKoo Biosciences, Inc.
An atypical antipsychotic that exhibits high affinity to serotonin 5HT2A (Ki =5.6 nM), dopamine D2 (Ki=6.3 nM) and D3 (Ki=7.1 nM) and noradrenaline α1 receptors (Ki=0.36 nM), moderate affinity for D4 (25 nM), 5HT6 (43 nM), 5HT7 (22 nM), and low affinity for 5HT1A (168 nM), D1 and histamine H1 receptors; is used for the treatment of schizophrenia.SchizophreniaApproved ......by ProbeChem
Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. ......by Selleck Chemicals LLC
Iloperidone is an atypical antipsychotic for the treatment of schizophrenia symptoms. Hoechst Marion Roussel Inc. made initial inquiries into the drug; however, in May 1996, they discontinued research, and in June 1997 gave research rights to Titan Pharmaceuticals. Titan then handed over worldwide development, manufacturing and marketing rights to Novartis in August 1998. On June 9, 2004, Titan Pharmaceuticals announced that the Phase III development rights have been acquired by Vanda Pharmaceuticals. FDA approved on May 9, 2009. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000016883

Storage condition

Solubility

DMSO 27 mg/mL; Water <1 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 27 mg/mL (63.3 mM); Ethanol4 mg/mL (9.37 mM); Water<1 mg/mL (<1 mM); In vivo 2% DMSO+40% PEG 300+dd H2O1.6mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Iloperidone Massachusetts General Hospital Depression 2012/4/30 2014/4/30 Phase 4 Clinical
Iloperidone Novartis AG Schizophrenia 2010/8/31 2011/12/31 Phase 4 Clinical
Iloperidone Novartis AG Schizophrenia 2011/2/28 2018/12/31 Phase 3 Clinical
Iloperidone New York State Psychiatric Institute 2012/11/30 2014/3/31 Phase 4 Clinical
Iloperidone Northwestern University Schizophrenia 2012/4/30 2015/12/31 Phase 4 Clinical
Iloperidone - Launched
7

Safety Data of Iloperidone

Hazard Symbols : F,T
Risk Statements : 11-23/24/25-39/23/24/25
Safety Statements : 16-36/37-45
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
AdooQ BioScience, LLC USA
Aladdin 10mg/RMB864();50mg/RMB3333() China
Apexbio Technology LLC USA
Axon Medchem BV 10mg/USD102(In Stock) Netherlands
Beijing Bode United Chemical Co., Ltd. China
Beijing Gaobo Pharm-Chemicals Tech. Co., Ltd CHINA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD62();50mg/USD240() USA
Carbosynth Limited 25mg/USD50()
Cayman Chemical Company USA
Chengdu Sino-Strong Pharmaceutical Co., Ltd. China
Chuzhou Baiao Biotechnology Co., Ltd. China
Cooper Chemical Co., Ltd. China
Langfang Gaobo Jingband Pharmaceutical Co., Ltd. China
Linyi Shengxin Pharmaceutical R&D Co., Ltd. China
MedChemexpress Co., Ltd. 10mg/USD62();50mg/USD240() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Pure Chemistry Scientific Inc. 10mg/USD52(In stock) USA
Santa Cruz Biotechnology, Inc. 10mg/USD135() USA
Selleck Chemicals LLC 10mg/USD70(In stock);10mM/1mLIn DMSO/USD90(In stock);50mg/USD270(In stock);100mg/USD470(In stock) USA
Shanghai DND Pharm-Technology Co., Inc. China
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD62();50mg/USD240() China
Taizhou Jiakang Chemical Co., Ltd. China
Target Molecule Corp. 2mg/USD24();10mg/USD68();50mg/USD152();100mg/USD240() USA
Thode Laboratories 10mg/USD120(In Stock) Canada
Tokyo Chemical Industry Co., Ltd. 25mg/USD37() Japan
10

Related Products

Other Forms of 133454-47-4

Name CAS No Formula MW
Iloperidone (hydrochloride) 1299470-39-5 C24H28ClFN2O4 462.94

Recommended Compounds in Dopamine Receptor 5-HT Receptor

Name CAS No Formula MW
SKF 38393 (hydrobromide) 20012-10-6 C16H18BrNO2 336.22
Ropinirole (hydrochloride) 91374-20-8 C16H25ClN2O 296.84
Fenoldopam 67227-56-9 C16H16ClNO3 305.76
Pergolide (mesylate) 66104-23-2 C20H30N2O3S2 410.59
Trifluoperazine (dihydrochloride) 440-17-5 C21H26Cl2F3N3S 480.42
Clomipramine (hydrochloride) 17321-77-6 C19H24Cl2N2 351.31
Dopamine (hydrochloride) 62-31-7 C8H12ClNO2 189.64
Domperidone 57808-66-9 C22H24ClN5O2 425.91
Pramipexole 104632-26-0 C10H17N3S 211.33
Chlorpromazine (hydrochloride) 69-09-0 C17H20Cl2N2S 355.33
Chlorprothixene 113-59-7 C18H18ClNS 315.86
Haloperidol (hydrochloride) 1511-16-6 C21H24Cl2FNO2 412.33
Risperidone (mesylate) 666179-96-0 C24H31FN4O5S 506.59
Risperidone (hydrochloride) 666179-74-4 C23H28ClFN4O2 446.95
Iloperidone (hydrochloride) 1299470-39-5 C24H28ClFN2O4 462.94
Ziprasidone 146939-27-7 C21H21ClN4OS 412.9356
Brexpiprazole 913611-97-9 C25H27N3O2S 433.57
Amisulpride (hydrochloride) 81342-13-4 C17H28ClN3O4S 405.94
L-DOPA 59-92-7 C9H11NO4 197.19
Cariprazine (hydrochloride) 1083076-69-0 C21H33Cl3N4O 463.87

Recommended Compounds in Same Indication

Name CAS No Formula MW
Rifabutin 72559-06-9 C46H62N4O11 847.0
Tianeptine 72797-41-2 C21H25ClN2O4S 436.95
Asenapine (maleate) 85650-56-2 C21H20ClNO5 401.84
Cariprazine 839712-12-8 C21H32Cl2N4O 427.41
PF-2545920 898562-94-2 C25H20N4O 392.45
lumateperone (Tosylate) 1187020-80-9 C31H36FN3O4S 565.6987
Lu AE58054 467459-31-0 C20H19F5N2O 398.37
EVP-6124 550999-75-2 C16H17ClN2OS 320.84
Asenapine 65576-45-6 C17H16ClNO 285.77
Adoprazine 222551-17-9 C24H24FN3O2 405.46
Vortioxetine 508233-74-7 C18H22N2S 298.45
Clozapine 5786-21-0 C18H19ClN4 326.82
Rolipram 61413-54-5 C16H21NO3 275.34
Bitopertin 845614-11-1 C21H20F7N3O4S 543.46
Bitopertin (R enantiomer) 845614-12-2 C21H20F7N3O4S 543.46
Zolpidem 82626-48-0 C19H21N3O 307.39
Lurasidone (Hydrochloride) 367514-88-3 C28H37ClN4O2S 529.14
Preladenant 377727-87-2 C25H29N9O3 503.56
Ziprasidone (hydrochloride monohydrate) 138982-67-9 C21H24Cl2N4O2S 467.41
Ziprasidone D8 1126745-58-1 C21H13D8ClN4OS 420.9849
11

Route of Synthesis

12

References

13

More Information

Iloperidone

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