您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Olanzapine
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Olanzapine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Olanzapine图片
CAS NO:132539-06-1
包装与价格:
包装价格(元)
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
奥氮平
LY170053
产品介绍
Olanzapine (LY170053) 是一种选择性的、具有口服活性的单胺能拮抗剂,高亲和力结合 5-羟色胺H1,5HT2A/2C,5HT3,5HT6(Ki分别为 7、4、11、57 和 5 nM),多巴胺D1-4(Ki=11-31 nM),毒蕈碱M1-5(Ki=1.9-25 nM) 和肾上腺素α1受体 (Ki=19 nM)。Olanzapine 是一种非典型的抗精神病剂。
生物活性

Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding toserotonin H1, 5HT2A/2C, 5HT3, 5HT6(Ki=7, 4, 11, 57, and 5 nM, respectively),dopamine D1-4(Ki=11 to 31 nM),muscarinic M1-5(Ki=1.9-25 nM), andadrenergic α1 receptor(Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].

IC50& Target[1]

5-HT2AReceptor

4 nM (Ki)

5-HT1Receptor

7 nM (Ki)

5-HT6Receptor

5 nM (Ki)

5-HT2CReceptor

11 nM (Ki)

5-HT3Receptor

57 nM (Ki)

Adrenergic α1 Receptor

19 nM (Ki)

Muscarinic M1-5 Receptor

1.9-25 nM (Ki)

Dopamine Receptor

 

Mitophagy

 

Apoptosis

 

体外研究
(In Vitro)

Olanzapine binds weakly to GABAA, Benzodiazepine (BZD), and β-adrenergic receptors (Ki>10 μM)[1][2].
Olanzapine induces autophagy in human SH-SY5Y neuronal cell line[3].
Olanzapine (1-100 μM for 144 h under serum starvation) results in a marked anti-proliferative effect in glioblastoma cell lines as well as glioma stem-like cells[4].
Olanzapine also enhances Temozolomide’s anti-tumor activity in glioblastoma cell lines[4].
Olanzapine induces apoptosis and necrosis in glioblastoma cell lines[4].

Cell Proliferation Assay[4]

Cell Line:U87MG and A172 glioblastoma cell lines as well as SC38 and SC40 glioma stem-like cells
Concentration:1, 10, 100 μM
Incubation Time:144 h; under serum starvation (1.5 % FBS) prior to performing MTT-assays
Result:Resulted in a marked antiproliferative effect with IC50values ranging from 25 to 79.9 μM. In U87MG cells, anchorage-independent growth was dose-dependently inhibited. In A172 cells, migration was also shown to be inhibited in a dose-dependent manner.

Western Blot Analysis[4]

Cell Line:U87MG and A172 cells
Concentration:10, 25, 50, and 100 μM
Incubation Time:7 h, 24 h, 48 h, 72 h
Result:Led to a dose responsive decrease of pAMPK expression after 72 h of treatment.
体内研究
(In Vivo)

Olanzapine (0.75, 1.5 and 3 mg/kg) evaluates body weight and periuterine fat mass, as well as insulin, non-esterified fatty acids, triglycerides, and glucose levels in mice[5]

Animal Model:Forty-two, 14, and 28 female CD-1 mice[5]
Dosage:0.75, 1.5 and 3 mg/kg
Administration:Orally and chronically administered; 35 days
Result:Increased body weight relative to vehicle on days 20-22, and from day 32 onwards there was a straightforward increase in body weight at 3 mg/kg. No differences were found between control and mice administered olanzapine at both 1.5 and 0.75 mg/kg.
Clinical Trial
分子量

312.43

性状

Solid

Formula

C17H20N4S

CAS 号

132539-06-1

中文名称

奥氮平;奥兰氮平;奥兰扎平

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 20 mg/mL(64.01 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.2007 mL16.0036 mL32.0072 mL
5 mM0.6401 mL3.2007 mL6.4014 mL
10 mM0.3201 mL1.6004 mL3.2007 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (6.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (6.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (6.40 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。