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Olanzapine/奥氮平 {[allProObj[0].p_purity_real_show]}

货号:A158972 同义名: LY170053

Olanzapine是一种多靶点拮抗剂,作用于 5-HT2A 受体和 D2 多巴胺受体,以及 muscarinic M3 受体。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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+
Olanzapine/奥氮平 化学结构 CAS号:132539-06-1
Olanzapine/奥氮平 化学结构
CAS号:132539-06-1
Olanzapine/奥氮平 3D分子结构
CAS号:132539-06-1
Olanzapine/奥氮平 化学结构 CAS号:132539-06-1
Olanzapine/奥氮平 3D分子结构 CAS号:132539-06-1
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Olanzapine/奥氮平 纯度/质量文件 产品仅供科研

货号:A158972 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 99%
Fluvoxamine maleate 99%
Iloperidone 99%
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 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 99%
Fluoxetine HCl 99.5%
Paroxetine HCl AChR 99%
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

95%
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 (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

98%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 99%
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%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

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

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
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

97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 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-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

95%
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

99%
Tetrahydroberberine +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 98% (HPLC)
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole HCl ++

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

99%
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 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

98%
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

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。

Olanzapine/奥氮平 生物活性

靶点
  • 5-HT2

  • D2 receptor

描述 Olanzapine is a D2 dopamine receptor antagonist with a high affinity for 5-HT2 serotonin. In vivo, sequential doses of olanzapine at 0.5, 3 and 10 mg/kg dose-dependently increased the extracellular dopamine (DA) and norepinephrine (NE) levels in all three brain areas. The increases appeared 30 min after olanzapine administration, reached peaks around 60 - 90 min and lasted for at least 2 h[3]. The high dose of olanzapine (10 mg/kg ) increased the number of fos-like positive nuclei in mesolimbic areas connected to the extended amygdala[4]. In vitro, olanzapine interacted with keyreceptorsof interest in schizophrenia, exihibiting a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors[5].

Olanzapine/奥氮平 细胞实验

Cell Line
Concentration Treated Time Description References
MIN6 cells 50 µM 14 hours Olanzapine partially inhibited mastoparan-induced insulin secretion Elife. 2020 Nov 17;9:e60970.
3T3-L1 adipocytes 5 µM 0, 12, 24, 48 and 72 hours Olanzapine inhibited insulin-stimulated glucose uptake over time, reaching maximum inhibition at 48 hours Sci Rep. 2019 Feb 7;9(1):1582.
HEK293T cells 150 µM 24 hours To evaluate the effect of olanzapine on mitophagy, results showed that olanzapine decreased the formation of mitolysosomes. Aging Cell. 2023 Nov;22(11):e14003.
HEK293T cells 150 µM 24 hours To evaluate the effect of olanzapine on mitochondrial parameters, results showed that olanzapine increased mitochondrial ROS levels, mitochondrial contents, and mitochondrial membrane potential. Aging Cell. 2023 Nov;22(11):e14003.
PC12 cells 0, 10, 20, 40 µM 24 hours To investigate whether olanzapine activated AMPK, results showed that olanzapine increased the phosphorylation of AMPK in both dose- and time-dependent manners Acta Pharmacol Sin. 2020 Apr;41(4):508-515.
U87 cells 0-400 µM 24, 48, 72 hours Evaluate the inhibitory effects of olanzapine on the growth of glioma cells, showing that olanzapine significantly inhibits the growth of glioma cells in a dose- and time-dependent manner. CNS Neurosci Ther. 2019 Sep;25(9):911-921.
LN229 cells 0-400 µM 24, 48, 72 hours Evaluate the inhibitory effects of olanzapine on the growth of glioma cells, showing that olanzapine significantly inhibits the growth of glioma cells in a dose- and time-dependent manner. CNS Neurosci Ther. 2019 Sep;25(9):911-921.
T98 cells 0-400 µM 24, 48, 72 hours Evaluate the inhibitory effects of olanzapine on the growth of glioma cells, showing that olanzapine significantly inhibits the growth of glioma cells in a dose- and time-dependent manner. CNS Neurosci Ther. 2019 Sep;25(9):911-921.
MIN6 cells 10-50 µM 4 hours or 14 hours Olanzapine inhibited glucose-stimulated insulin secretion in a concentration-dependent manner Elife. 2020 Nov 17;9:e60970.
PC12 cells 20 µM 48 hours To investigate the effect of olanzapine on autophagy, results showed that olanzapine induced autophagy and increased autophagic vacuoles Acta Pharmacol Sin. 2020 Apr;41(4):508-515.
3T3-L1 adipocytes 0, 1, 2, 5, or 10 µM 48 hours Olanzapine dose-dependently inhibited insulin-stimulated glucose uptake, increased NF-κB activity and decreased IκBα protein expression Sci Rep. 2019 Feb 7;9(1):1582.

Olanzapine/奥氮平 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c mice and Sprague Dawley rats Insulin resistance model Intraperitoneal injection 10 mg/kg Once daily for 8 weeks Chronic olanzapine treatment caused metabolic symptoms, including insulin resistance, by markedly elevating plasma pro-inflammatory cytokine levels Sci Rep. 2019 Feb 7;9(1):1582.
Caenorhabditis elegans Wild-type N2 Administered via NGM medium 25, 50, 100, 150, 300 μM From the L4 larval stage until death To evaluate the effect of olanzapine on lifespan, results showed that olanzapine significantly shortened the lifespan of C. elegans. Aging Cell. 2023 Nov;22(11):e14003.
Mice BALB/c mice Oral 3 mg/kg/day or 10 mg/kg/day Once a day for 1-6 weeks Olanzapine induced proinsulin misfolding in mouse islets Elife. 2020 Nov 17;9:e60970.
Female Sprague-Dawley rats Methylazoxymethanol (MAM)-induced neurodevelopmental model of schizophrenia Intramuscular injection 5 mg/kg Acute administration, observed over 24 hours To investigate the acute metabolic effects of olanzapine and haloperidol in the MAM model, finding that olanzapine induced pronounced serum lipid profile alterations in MAM rats, while haloperidol had weaker metabolic effects. CNS Neurosci Ther. 2024 Feb;30(2):e14565
Wistar rats Chronic social isolation model Intraperitoneal injection 7.5 mg/kg/day Once daily for 3 weeks To investigate the effects of Olz on the number of PV+ and GAD67+ cells in the hippocampus of CSIS rats and its antioxidative and anti-inflammatory potential. Olz reversed CSIS-induced depressive-like behavior, increased the number of GAD67+ cells in the SO and SP layers of dCA1, reduced the number of PV+ and GAD67+ cells in the SR layer of dCA3, and modulated oxidative stress and inflammatory markers. Int J Mol Sci. 2023 Dec 6;24(24):17181

Olanzapine/奥氮平 参考文献

[1]Cipriani A, Rendell JM, et al. Olanzapine in long-term treatment for bipolar disorder. Cochrane Database Syst Rev. 2009 Jan 21;(1):CD004367.

[2]Bymaster FP, Rasmussen K, et al. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug. J Clin Psychiatry. 1997;58 Suppl 10:28-36.

[3]Li XM, Perry KW, Wong DT, Bymaster FP. Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum. Psychopharmacology (Berl). 1998;136(2):153-161.

[5]Bymaster FP, Rasmussen K, Calligaro DO, et al. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug. J Clin Psychiatry. 1997;58 Suppl 10:28-36.

Olanzapine/奥氮平 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.00mL

3.20mL

1.60mL

32.01mL

6.40mL

3.20mL

Olanzapine/奥氮平 技术信息

CAS号132539-06-1
分子式C17H20N4S
分子量 312.43
SMILES Code CC1=CC(C(N2CCN(C)CC2)=N3)=C(S1)NC4=C3C=CC=C4
MDL No. MFCD00866702
别名 LY170053
运输蓝冰
InChI Key KVWDHTXUZHCGIO-UHFFFAOYSA-N
Pubchem ID 135398745
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

DMSO: 18 mg/mL(57.61 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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