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伊潘立酮 /Iloperidone {[allProObj[0].p_purity_real_show]}

货号：A855415 同义名： HP 873

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

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Iloperidone 化学结构 CAS号：133454-47-4
Iloperidone 化学结构
CAS号：133454-47-4
Iloperidone 3D分子结构
CAS号：133454-47-4
Iloperidone 化学结构 CAS号：133454-47-4
Iloperidone 3D分子结构 CAS号：133454-47-4
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Iloperidone 纯度/质量文件 产品仅供科研

货号：A855415 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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更多 >
产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		98%
Venlafaxine ✔ 98%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 98%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 98%
Fluoxetine HCl ✔ 99.5%
Paroxetine hydrochloride ✔ AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		98%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		99%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		98%
Tropisetron ✔ 99%
Palonosetron ✔ 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron hydrochloride dihydrate ✔ 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		98%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 D1 receptor ↓ D2 receptor ↓ D3 receptor ↓ D4 receptor ↓ D5 receptor ↓ DAT ↓ Dopamine receptor ↓ 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

 		98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 95%
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		98%
Levosulpiride ✔ 99+%
Pridopidine ✔ 95%
Metoclopramide ✔ ✔ 99+%
Molindone HCl ✔ 98%
Sulpiride ✔ 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		98+%
Phenothiazine ✔ 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		98%
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		98%
Domperidone ✔ 99+%
ONC206 ✔ 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

 		++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		98%
MPP+ iodide ✔ 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		97%
Benztropine mesylate ++

DAT, IC50: 118 nM

 		98%
Azaperone ✔ 98%
Ziprasidone HCl ✔ 98+%
Paliperidone ✔ 98%
Alizapride HCl ✔ 99+%
Amisulpride ✔ 98%
Quetiapine hemifumarate ✔ Adrenergic Receptor 98%
Clozapine N-oxide ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Iloperidone 生物活性

靶点

  • 5-HT
描述 Iloperidone is a second generation (atypical) antipsychotic agent that is used for treatment of schizophrenia[3]. 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)[4]. Iloperidone concentration-dependently inhibited hERG 1A/3.1 currents by preferentially interacting with the open states of channels, but not by the disruption of membrane trafficking or surface membrane expression of hERG 1A and hERG 1A/3.1 channel proteins[5]. Iloperidone directly inhibits Kv channels in a concentration- and use (state)-dependent manner independently of its antagonism of serotonin and dopamine receptors. Furthermore, the primary target of iloperidone is the Kv1.5 subtype[6]. 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[7].

Iloperidone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02191358 - Completed - United States, California ... 展开 >> Dr. Michael Dao Garden Grove, California, United States, 92844 United States, Colorado Kaiser Permanente Colorado Denver, Colorado, United States, 80011 United States, Kentucky Gill Heart Institute Lexington, Kentucky, United States, 40508 United States, Maryland IRC Clinics Towson, Maryland, United States, 21204 United States, Massachusetts Internal Medicine & Cardiology Associates Fall River, Massachusetts, United States, 02720 Prima CARE Fall River, Massachusetts, United States, 02720 United States, Virginia Carilion Clinic Christiansburg, Virginia, United States, 24073 收起 <<
NCT03373461 IgA Nephropathy Phase 2 Recruiting April 6, 2021 Australia, New South Wales ... 展开 >> Novartis Investigative Site Recruiting Westmead, New South Wales, Australia, 2145 Australia, Victoria Novartis Investigative Site Recruiting Melbourne, Victoria, Australia, 3050 Belgium Novartis Investigative Site Recruiting Edegem, Antwerpen, Belgium, 2650 Novartis Investigative Site Recruiting Leuven, Belgium, 3000 Novartis Investigative Site Recruiting Roeselare, Belgium, 8800 Denmark Novartis Investigative Site Recruiting Aalborg, Denmark, 9000 Finland Novartis Investigative Site Recruiting HUS, Finland, 00029 Netherlands Novartis Investigative Site Recruiting Groningen, Netherlands, 9713 GZ Norway Novartis Investigative Site Recruiting Bergen, Norway, 5021 Novartis Investigative Site Recruiting Loerenskog, Norway, NO-1478 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 119228 Novartis Investigative Site Recruiting Singapore, Singapore, 169608 Sweden Novartis Investigative Site Recruiting Stockholm, Sweden, 141 86 Taiwan Novartis Investigative Site Recruiting New Taipei City, Taiwan, 23561 Novartis Investigative Site Recruiting Taichung, Taiwan, 40705 Thailand Novartis Investigative Site Recruiting Bangkok, Thailand, 10400 United Kingdom Novartis Investigative Site Recruiting Cambridge, Cambrigdeshire, United Kingdom, CB2 0QQ Novartis Investigative Site Recruiting Leicester, United Kingdom, LE5 4PW Novartis Investigative Site Recruiting London, United Kingdom, SE5 9RS Novartis Investigative Site Recruiting London, United Kingdom, W12 0HS Novartis Investigative Site Recruiting Newcastle Upon Tyne, United Kingdom, NE7 7DN 收起 <<
NCT02600741 - Completed - -

Iloperidone 参考文献

[1]Kalkman HO, Subramanian N, et al. Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. Neuropsychopharmacology. 2001 Dec;25(6):904-14.

[2]Kongsamut S, Roehr JE, et al. Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23.

[3]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Iloperidone. 2018 Apr 15

[4]Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A. Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23

[5]Lee HJ, Choi BH, Choi JS, Hahn SJ. Effects of iloperidone on hERG 1A/3.1 heterotetrameric channels. Neuroreport. 2021 Nov 2;32(16):1299-1306

[6]An JR, Seo MS, Jung HS, Kang M, Heo R, Bae YM, Han ET, Yang SR, Park WS. Inhibition of voltage-dependent K+ channels by iloperidone in coronary arterial smooth muscle cells. J Appl Toxicol. 2020 Sep;40(9):1297-1305

[7]Sainati SM, Hubbard JW, Chi E, Grasing K, Brecher MB. Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol. 1995 Jul;35(7):713-20

Iloperidone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.72mL

2.34mL

1.17mL

23.45mL

4.69mL

2.34mL

Iloperidone 技术信息

CAS号133454-47-4
分子式C24H27FN2O4
分子量 426.481
别名 HP 873
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(117.24 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Iloperidone | 133454-47-4 | HP 873 | HP873 | HP-873 | 5-HT Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | 5-HT Receptor | Dopamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Iloperidone 纯度/质量文件 | Iloperidone 亚型比较 | Iloperidone 生物活性 | Iloperidone 临床数据 | Iloperidone 参考文献 | Iloperidone 实验方案 | Iloperidone 技术信息

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