Orlistat (Ro 18-0647)

For research use only. Not for use in humans.

目录号:S1629 别名: Tetrahydrolipstatin 中文名称:奥利司他

Orlistat (Ro 18-0647) Chemical Structure

CAS No. 96829-58-2

Orlistat (Ro 18-0647, Tetrahydrolipstatin) 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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1053.71 现货
RMB 812.99 现货
RMB 2187.46 现货
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客户使用Selleck生产的Orlistat (Ro 18-0647)发表文献6篇:

产品安全说明书

Lipase抑制剂选择性比较

生物活性

产品描述 Orlistat (Ro 18-0647, Tetrahydrolipstatin) 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
lipase [1]
(Cell-free assay)
Fatty acid synthesis [1]
(Cell-free assay)
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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N18TG2 NV6zZ3Q2TnWwY4Tpc44h[XO|YYm= MlnqNlAhdWmwcx?= Ml3KTY5pcWKrdHnvckBw\iCGQVfMZYxxcGFiaX6gcY92e2ViTkG4WGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbY9vd227Y3nuMYlv\HWlZXSg[o9zdWG2aX;uJI9nKDJvQVegbY5kfWKjdHXkJIZweiB{MDDtbY5{KGK7IFzDMW1UKGGwYXz5d4l{NCCLQ{WwJF0hOC5yMjFOwG0v M3:zNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUG3NlIyLz5{NkmxO|IzOTxxYU6=
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HEK293 NV3oc451TnWwY4Tpc44h[XO|YYm= MknVTY5pcWKrdHnvckBw\iCqdX3hckBCSkiGNjDjc451[WmwaX7nJJBEVVZ4LVHDMYhCSkiGNjD0doFve2[nY4Tl[EBqdnSxIFjFT|I6OyClZXzsd{whUUN3MDC9JFAvODR5OE[g{txONg>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd3Mkm4Nkc,OjV5NUK5PFI9N2F-
HEK293 MkLmSpVv[3Srb36gZZN{[Xl? MWDJcohq[mm2aX;uJI9nKGi3bXHuJGFDUER4IHPvcpRicW6rbnegdGNOXjZvQVOtbGFDUER4IITyZY5{\mWldHXkJIlvfG9iSFXLNlk{KGOnbHzzMEBKSzVyIE2gNE4xPDhizszNMi=> NVTnVlRsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OVI6QDJpPkK1O|UzQTh{PD;hQi=>
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COS7 MofYSpVv[3Srb36gZZN{[Xl? MknRTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDERWdN[mW2YTDveoVz\XiycnXzd4VlKGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNQWzdiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJI9nKDJvYYLhZ4hq\G:wb4ns[4x6[2W{b3ygZpkhX2W|dHXyckBjdG:2dHnu[y=> M3nRPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkW3PVcyLz5zOE[1O|k4OTxxYU6=
COS7 Ml3kSpVv[3Srb36gZZN{[Xl? MVvJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IFTBS2xidHCqYTDveoVz\XiycnXzd4VlKGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNQWzdiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJI9nKDJvYYLhZ4hq\G:wb4ns[4x6[2W{b3ygZpkhX2W|dHXyckBjdG:2dHnu[y=> NYG2eGdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2OVc6PzFpPkG4OlU4QTdzPD;hQi=>
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HEK293 MXPGeY5kfGmxbjDhd5NigQ>? M4rSPFEhfU1? NWDVeZF4OTBibXnudy=> MVvS[ZZmenOrYnzlJIlvcGmkaYTpc44hd2ZiaIXtZY4hSUKKRE[g[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDheEAyKHWPIIDy[U1qdmO3YnH0[YQh\m:{IEGwJI1qdnNiYnXmc5JmKDJvQVegd5Vje3S{YYTlJIFl\Gm2aX;uJIZwdGyxd3XkJIJ6KHKjcHnkJFQxKG[xbHSgZ49ueG:3bnSg[IltfXSrb36gcYVie3W{ZXSgZYZ1\XJiMUCgeI8hQTBibXnud{BjgSCKUFzDJI1mfGixZB?= M3X0U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{S0OVk3Lz5{NkO0OFU6PjxxYU6=
LNCAP NYLVZlRqTnWwY4Tpc44h[XO|YYm= M4LvU|IxKHWP MU[0PEBpenN? NYXxclFtUW6mdXP0bY9vKG:oIHPoc4xme3Sncn;sJI1mfGGkb3zpd40h\GW{ZXf1cIF1cW:wIHnuJIh2dWGwIFzOR2FRKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDORmQu[2ixbHXzeIVzd2xidYD0ZYtmKGG2IEKwJJVOKGGodHXyJFQ5KGi{czDifUBFSVCLL1Hs[ZhiKG[udX;yJFY{OyCyaHHscI9q\GmwIIP0ZYlvcW6pIHLhd4VlKGirZ3itZ49vfGWwdDDpcYFocW6pIHHuZYx6e2m| MlLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2N{SwO|EoRjJ7NEe0NFcyRC:jPh?=
BV2 MkC1SpVv[3Srb36gZZN{[Xl? NHHqbGs{OCCvaX7z NEj5c3FKdmirYnn0bY9vKG:oIFHCTGQ3KGmwIH3veZNmKEKYMjDj[YxteyCycnXpcoN2[mG2ZXSg[o9zKDNyIH3pcpMh[W6mIIP1ZpNmeXWnboSgZYRlcXSrb36gc4YhYzOKXT2yMW9IKHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pIH3leIhw\A>? NEn3VFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4OFg3OSd-MkiyPFQ5PjF:L3G+
BV2 M2W5R2Z2dmO2aX;uJIF{e2G7 NECyeI4{OCCvaX7z MkPqTY5pcWKrdHnvckBw\iCDQljENVIhcW5ibX;1d4UhSlZ{IHPlcIx{KHC{ZXnuZ5Vj[XSnZDDmc5IhOzBibXnud{BidmRic4Xid4VyfWWwdDDh[IRqfGmxbjDv[kBcO0ifLUKtU2che3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFE2KG2rboOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmdibXX0bI9l MmHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OES4OlEoRjJ6Mki0PFYyRC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
FASN / AR / p-AKT / p-p53 / p53 / VEGF / Cyclin D1 / Bcl-2 / Cleaved caspase-3 ; 

PubMed: 31527721     


Orlistat reduced the expressions of FASN, pAkt, VEGF, cyclin D1, and Bcl-2 in both cell lines. Decreased androgen receptor (AR) and elevated p-p53/p53 levels were found in LNCaP cells after orlistat treatment. 

31527721
Growth inhibition assay
Cell viability; 

PubMed: 28387458     


PC3, DU145, and LNCaP cells were treated with varying doses of Orlistat (0–300 uM) for 24 h. MTT assay was used to determine cell viability. Values are mean ± S.E.M (n = 3). *, p < 0.05 versus control.

28387458
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: Jurkat CD4+ T cell leukemia cell line
  • Concentrations: 2.5, 5, 10, 20, 40 μM
  • Incubation Time: 2天
  • Method:

    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。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: Nude mice (PC-3 xenograft tumor)
  • Dosages: 240 mg/kg/day
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 99 mg/mL (199.7 mM)
Water Insoluble
Ethanol '99 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
13mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 495.73
化学式

C29H53NO5

CAS号 96829-58-2
储存条件 粉状
溶于溶剂
别名 Tetrahydrolipstatin

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01755676 Completed Drug: Orlistat 60 mg|Other: Placebo Obesity EMS September 2016 Phase 3
NCT02141230 Withdrawn Drug: Alli® 60 mg Weight Loss GlaxoSmithKline|Hamell December 2015 Not Applicable
NCT01719419 Withdrawn Drug: Placebo|Drug: Orlistat Overweight Pennington Biomedical Research Center March 2012 Not Applicable
NCT01332448 Completed Drug: Orlistat 120|Drug: Orlistat 60 Obesity GlaxoSmithKline February 2010 --
NCT01414465 Completed Drug: Orlistat Overweight University of Campinas Brazil|Germed Pharma October 2009 Not Applicable
NCT01170806 Completed Drug: Orlistat Obesity University of Campinas Brazil|Germed Pharma October 2009 Not Applicable

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID