Orlistat
别名: Tetrahydrolipstatin,Ro 18-0647 中文名称：奥利司他
Orlistat是一种通用的脂肪酶 lipase 抑制剂，作用于人体十二指肠液的PL，IC50为122 ng/ml。Orlistat 处理可抑制细胞增殖、诱导凋亡并阻滞细胞周期。
Orlistat Chemical Structure
CAS: 96829-58-2
客户使用Selleck的发表文献14篇
产品质控
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Lipase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HEK293 | Function assay | 1 uM | 10 mins | Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 10 mins by HPLC method, IC50 = 0.01318 μM. | 26344596 |
| HEK293 | Function assay | 1 uM | 10 mins | Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 30 mins by HPLC method, IC50 = 0.01413 μM. | 26344596 |
| HEK293 | Function assay | 1 uM | 10 mins | Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 60 mins by HPLC method, IC50 = 0.01995 μM. | 26344596 |
| HEK293 | Function assay | 1 uM | 10 mins | Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 90 mins by HPLC method, IC50 = 0.03715 μM. | 26344596 |
| MDA-MB-435 | Apoptosis assay | 25 uM | 72 hrs | Induction of apoptosis in human MDA-MB-435 cells assessed as DNA fragmentation at 25 uM after 72 hrs | 18710210 |
| HEK293 | Function assay | 1 uM | 10 mins | Reversible inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 10 to 90 mins by HPLC method | 26344596 |
| LNCAP | Function assay | 20 uM | 48 hrs | Induction of cholesterol metabolism deregulation in human LNCAP cells assessed as reduction in NBD-cholesterol uptake at 20 uM after 48 hrs by DAPI/Alexa fluor 633 phalloidin staining based high-content imaging analysis | 29474071 |
| COS7 | Function assay | 20 mins | Inhibition of recombinant human HL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.003 μM. | 30613337 | |
| COS | Function assay | 15 mins | Inhibition of human recombinant DAGLalpha expressed in African green monkey COS cells using sn-1-stearoyl-2-[14C]-arachidonoyl-glycerol as substrate incubated for 15 mins by beta counting analysis, IC50 = 0.001 μM. | 26917221 | |
| HT1080 | Function assay | 20 mins | Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.006 μM. | 30613337 | |
| HEK293F | Function assay | 20 mins | Inhibition of recombinant human PL expressed in HEK293F cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.006 μM. | 30613337 | |
| N18TG2 | Function assay | 20 mins | Inhibition of DAGLalpha in mouse N18TG2 cells assessed as inhibition of ionomycin-induced formation of 2-AG incubated for 20 mins by LC-MS analysis, IC50 = 0.02 μM. | 26917221 | |
| COS7 | Function assay | 20 mins | Inhibition of recombinant human LPL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay, IC50 = 0.066 μM. | 30613337 | |
| HEK293 | Function assay | 10 mins | Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method, IC50 = 0.19 μM. | 26344596 | |
| HEK293 | Function assay | 10 mins | Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method, IC50 = 0.19055 μM. | 26344596 | |
| BxPC3 | Function assay | 10 to 14 days | Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay, IC50 = 8.45 μM. | 25513712 | |
| MDA-MB-435 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay, IC50 = 16.8 μM. | 18710210 | |
| HepG2 (DPX-2) | Function assay | 24 hrs | Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50 = 28.2 μM. | 20966043 | |
| BV2 | Function assay | 30 mins | Inhibition of ABHD6 in mouse BV2 cells preincubated for 30 mins and subsequent addition of [3H]-2-OG substrate measured after 15 mins by liquid scintillation counting method | 28284861 | |
| BV2 | Function assay | 30 mins | Inhibition of ABHD12 in mouse BV2 cells preincubated for 30 mins and subsequent addition of [3H]-2-OG substrate measured after 15 mins by liquid scintillation counting method | 28284861 | |
| HEK293T | Function assay | Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay, IC50=0.01 μM | 22738638 | ||
| HEK293T | Function assay | Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe, IC50 = 0.03 μM. | 18657971 | ||
| HEK293 | Function assay | Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells, IC50 = 0.04786 μM. | 25752982 | ||
| HEK293 | Function assay | Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells, IC50 = 0.048 μM. | 25752982 | ||
| HEK293T | Function assay | Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe, IC50 = 0.05 μM. | 18657971 | ||
| COS7 | Function assay | Inhibition of human recombinant DAGLalpha overexpressed in african green monkey COS7 cells, IC50 = 0.06 μM. | 18657971 | ||
| COS7 | Function assay | Inhibition of human recombinant DAGLbeta overexpressed in african green monkey COS7 cells, IC50 = 0.06 μM. | 18657971 | ||
| HEK293T | Function assay | Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe, IC50 = 0.08 μM. | 18657971 | ||
| HEK293 | Function assay | Inhibition of human ABHD12 containing pCMV6-XL4-hABHD12 transfected into HEK293 cells, IC50 = 0.19 μM. | 25752982 | ||
| HEK293 | Function assay | Inhibition of human ABHD12 containing pCMV6-XL4-hABHD12 transfected into HEK293 cells, IC50 = 0.19055 μM. | 25752982 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells by scintillation counting, Ki = 2.5 μM. | 18831576 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability, IC50 = 13 μM. | 29541373 | ||
| COS7 | Function assay | Inhibition of recombinant DAGLbeta overexpressed in african green monkey COS7 cells assessed as accumulation of 2-arachidonoylglycerol by Western blotting | 18657971 | ||
| COS7 | Function assay | Inhibition of recombinant DAGLalpha overexpressed in african green monkey COS7 cells assessed as accumulation of 2-arachidonoylglycerol by Western blotting | 18657971 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Orlistat是一种通用的脂肪酶 lipase 抑制剂，作用于人体十二指肠液的PL，IC50为122 ng/ml。Orlistat 处理可抑制细胞增殖、诱导凋亡并阻滞细胞周期。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Orlistat是一种脂肪酶和脂肪酸合成酶抑制剂，常被用于长期治疗肥胖，口服途径。Orlistat在体外对癌细胞具有抗增殖活性，提高促凋亡NOXA蛋白水平[1]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | Jurkat CD4+ T cell leukemia cell line | ||
| 浓度 | 2.5, 5, 10, 20, 40 μM | |||
| 孵育时间 | 2天 | |||
| 方法 | 将不同浓度的药物加入白血病细胞中进行孵育，处理2天。药物处理完后，溶液细胞并进行WB分析。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | FASN / AR / p-AKT / p-p53 / p53 / VEGF / Cyclin D1 / Bcl-2 / Cleaved caspase-3 |
|
31527721 | |
| Growth inhibition assay | Cell viability |
|
28387458 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 通过口服途径进行Orlistat给药，药物甚少被胃肠道吸收，能够抑制大部分脂质的吸收、可减少外源脂质供应。由于orlistat的口服生物利用度低，其效用局限于胃肠道，在胃肠道使胰腺脂肪酶失活。因此，如果要靶向乳腺、前列腺等肿瘤，其配方和给药途径需要改变。Orlistat抑制肿瘤细胞的增殖、诱导肿瘤细胞凋亡、抑制裸鼠中PC-3肿瘤的生长。给药浓度为155 mg/kg时，在小鼠中对Orlistat进行药代动力学分析，通过腹腔注射给药，将在给药后2小时后达到血液峰浓度（~10 μM），而这个时间段后，血药浓度迅速衰减[2]。 | |
|---|---|---|
| 动物实验 | Animal Models | Nude mice (PC-3 xenograft tumor) |
| Dosages | 240 mg/kg/day | |
| Administration | i.p. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01755676 | Completed | Obesity |
EMS |
September 2016 | Phase 3 |
| NCT02141230 | Withdrawn | Weight Loss |
GlaxoSmithKline|Hamell |
December 2015 | Not Applicable |
| NCT01719419 | Withdrawn | Overweight |
Pennington Biomedical Research Center |
March 2012 | Not Applicable |
| NCT01332448 | Completed | Obesity |
GlaxoSmithKline |
February 2010 | -- |
| NCT01414465 | Completed | Overweight |
University of Campinas Brazil|Germed Pharma |
October 2009 | Not Applicable |
化学信息&溶解度
| 分子量 | 495.73 | 分子式 | C29H53NO5 |
| CAS号 | 96829-58-2 | SDF | Download Orlistat SDF |
| Smiles | CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 99 mg/mL ( (199.7 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 99 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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