Iloperidone | HP 873 | 5-HT Receptor Antagonist | AmBeed-信号通路专用抑制剂

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伊潘立酮 /Iloperidone 99%+

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
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

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： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

5-羟色胺受体亚型比较
多巴胺受体亚型比较

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 (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM								99%+
Venlafaxine	✔								99%+
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%+
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								99%+
Trazodone	✔								98+%
Clomipramine HCl	✔								99%+
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								99%+
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								99%+
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								99%+
Latrepirdine 2HCl	✔							GluR	99%+
Fluoxetine hydrochloride	✔								98%
Paroxetine hydrochloride	✔							AChR	99%+
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 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						99%+
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			✔						99%+
Clozapine			✔						99%+
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					99%+
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					99%+
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-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		99%+
Risperidone		++ 5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM	++++ 5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		99%+
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-HT1B, pKi: 6.1 5-HT1D, pKi: 6	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 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		✔							98%+
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		✔							99%+
Sulpiride		✔							99+%
Perospirone		++++ D2 receptor, Ki: 1.4 nM							99%
Perospirone HCl		++++ D2 receptor, Ki: 1.4 nM							98+%
Phenothiazine		✔							99%+
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						99%+
Domperidone		✔							99+%
ONC206		✔							99%+
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				99%+
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			99%+
Azaperone							✔		99%+
Ziprasidone HCl							✔		98+%
Paliperidone							✔		99%+
Alizapride HCl							✔		99+%
Amisulpride							✔		99%+
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

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

液体 -20°C:3-6个月-80°C:12个月

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

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	-	-
NCT03565068	Schizophrenia	Phase 1	Suspended(Study is on hold pen... 展开 >>ding evaluation of emerging preclinical findings) 收起 <<	October 9, 2019	United States, California ... 展开 >> California Clinical Trials ( Site 0001) Glendale, California, United States, 91206 收起 <<
NCT02181803	Schizophrenia	Phase 1	Completed	-	-
NCT01498770	-		Completed	-	-
NCT00254202	Schizophrenia	Phase 3	Completed	-	-
NCT00806234	-		Completed	-	-
NCT03420534	Bioequivalence	Phase 1	Active, not recruiting	March 14, 2018	China, Henan ... 展开 >> The first affiliated hospital of zhengzhou university. Zhengzhou, Henan, China, 450000 收起 <<
NCT02453893	Schizophrenia	Phase 3	Unknown	-	China, Shanghai ... 展开 >> Shanghai Mental Health Center Recruiting Shanghai, Shanghai, China, 200030 Contact: Li Hua fang, Ph.D 86-021-34773128 收起 <<
NCT00806234	Psychotic Disorders	Phase 4	Completed	-	United States, Maryland ... 展开 >> University of Maryland Baltimore, Maryland, United States, 21201 Johns Hopkins Hospital Baltimore, Maryland, United States, 21205 United States, New York The Zucker Hillside Hospital Glen Oaks, New York, United States, 11004 United States, North Carolina University of North Carolina, Division of Child and Adolescent Psychiatry Chapel Hill, North Carolina, United States, 27599 收起 <<
NCT01686815	-		Unknown	December 2015	United States, Massachusetts ... 展开 >> Freedom Trail Clinic Recruiting Boston, Massachusetts, United States, 02114 Contact: Liana J Petruzzi, BA 617-912-7882 lpetruzzi@partners.org Contact: Leah N Briggs, BS 617-912-7848 lbriggs@partners.org Principal Investigator: David C Henderson, MD 收起 <<
NCT01291511	Schizophrenia	Phase 3	Completed	-	-
NCT01464229	-		Completed	-	-
NCT01464229	Major Depressive Disorder	Phase 4	Completed	-	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 收起 <<
NCT01623713	Schizophrenia ... 展开 >> Iloperidone Efficacy 收起 <<	Phase 2	Completed	-	China, Beijing ... 展开 >> Sixth Hospital of Peking University Peking, Beijing, China, 100191 收起 <<
NCT01920802	-		Completed	-	-
NCT01920802	Healthy	Phase 4	Completed	-	United States, New York ... 展开 >> New York State Psychiatric Institute New York, New York, United States, 10032 收起 <<
NCT01929889	Schizophrenia ... 展开 >> Schizoaffective Disorder 收起 <<	Phase 4	Terminated(Low recruitment)	-	United States, Illinois ... 展开 >> Northwestern University Chicago, Illinois, United States, 60611 收起 <<
NCT01929889	-		Terminated(Low recruitment)	-	-
NCT01917318	Post Traumatic Stress Disorder	Phase 2	Completed	-	United States, Colorado ... 展开 >> University of Colorado Depression Center; Clinical and Translational Research Center (CTRC) Aurora, Colorado, United States, 80045 收起 <<
NCT01348100	Schizophrenia	Phase 1 Phase 2	Completed	-	United States, California ... 展开 >> Novartis Investigative Site Glendale, California, United States, 91206 United States, Pennsylvania Novartis Investigative Site Philadelphia, Pennsylvania, United States, 19149 收起 <<
NCT01348100	-		Completed	-	-
NCT01529294	Hepatic Impairment	Phase 1	Completed	-	United States, California ... 展开 >> Novartis Investigative Site Anaheim, California, United States, 92801 United States, Florida Novartis Investigative Site Miami, Florida, United States, 33169 Novartis Investigative Site Orlando, Florida, United States, 32809 Novartis Investigative Site South Miami, Florida, United States, 33143 收起 <<
NCT01495169	Safety and Tolerability of Ilo... 展开 >>peridone 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> Novartis Investigative Site Costa Mesa, California, United States, 92626 United States, Florida Novartis Investigative Site North Miami, Florida, United States, 33161 United States, Georgia Novartis Investigative Site Atlanta, Georgia, United States, 30308 United States, Idaho Novartis Investigative Site Coeur d'Alene, Idaho, United States, 83814 United States, Maryland Novartis Investigative Site Baltimore, Maryland, United States, 21205 United States, Missouri Novartis Investigative Site St. Louis, Missouri, United States, 63044 United States, New Jersey Novartis Investigative Site Marlton, New Jersey, United States, 08053 United States, Ohio Novartis Investigative Site Cincinnati, Ohio, United States, 45219 Novartis Investigative Site Cleveland, Ohio, United States, 44106-5000 United States, Utah Novartis Investigative Site Salt Lake City, Utah, United States, 84106 收起 <<
NCT02413918	Bipolar Disorder	Phase 4	Completed	-	United States, Texas ... 展开 >> UT Health Science Center San Antonio San Antonio, Texas, United States, 78229 收起 <<
NCT02413918	-		Completed	-	-
NCT01207414	-		Completed	-	-
NCT01207414	Schizophrenia	Phase 4	Completed	-	-

伊潘立酮 /Iloperidone 99%+

Iloperidone 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Iloperidone 质控信息

Iloperidone 生物活性

Iloperidone 临床研究

Iloperidone 参考文献

Iloperidone 实验方案

Iloperidone 技术信息

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Iloperidone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Iloperidone 质控信息

Iloperidone 生物活性

Iloperidone 临床研究

Iloperidone 参考文献

Iloperidone 实验方案

Iloperidone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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