Orlistat

別名: Tetrahydrolipstatin,Ro 18-0647 中文名稱：奧利司他

目錄號：S1629 Purity: 99.91%

Orlistat是一種通用的脂肪酶 lipase 抑制劑，作用于人體十二指腸液的PL，IC50為122 ng/ml。Orlistat 處理可抑制細胞增殖、誘導(dǎo)凋亡并阻滯細胞周期。

Orlistat Chemical Structure

CAS: 96829-58-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1053.71	現(xiàn)貨
25mg	812.99	現(xiàn)貨
100mg	2187.46	現(xiàn)貨
1g	7944.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.91%

99.91

Orlistat相關(guān)產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

lipase ^[1]
(Cell-free assay)

Fatty acid synthesis ^[1]
(Cell-free assay)

體外研究(In Vitro)
體外研究活性	Orlistat是一種脂肪酶和脂肪酸合成酶抑制劑，常被用于長期治療肥胖，口服途徑。Orlistat在體外對癌細胞具有抗增殖活性，提高促凋亡NOXA蛋白水平^[1]。
細胞實驗	細胞系	Jurkat CD4+ T cell leukemia cell line
	濃度	2.5, 5, 10, 20, 40 μM
	孵育時間	2天
	方法	將不同濃度的藥物加入白血病細胞中進行孵育，處理2天。藥物處理完后，溶液細胞并進行WB分析。
實驗圖片	檢測方法	檢測指標	實驗圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	通過口服途徑進行Orlistat給藥，藥物甚少被胃腸道吸收，能夠抑制大部分脂質(zhì)的吸收、可減少外源脂質(zhì)供應(yīng)。由于orlistat的口服生物利用度低，其效用局限于胃腸道，在胃腸道使胰腺脂肪酶失活。因此，如果要靶向乳腺、前列腺等腫瘤，其配方和給藥途徑需要改變。Orlistat抑制腫瘤細胞的增殖、誘導(dǎo)腫瘤細胞凋亡、抑制裸鼠中PC-3腫瘤的生長。給藥濃度為155 mg/kg時，在小鼠中對Orlistat進行藥代動力學(xué)分析，通過腹腔注射給藥，將在給藥后2小時后達到血液峰濃度（~10 μM），而這個時間段后，血藥濃度迅速衰減^[2]。
動物實驗	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
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[1] Cioccoloni G, et al. Int J Oncol. 2015, 47(2):764-72. [2] Kridel SJ, et al. Cancer Res. 2004, 64(6):2070-5.

參考文獻

[1] Cioccoloni G, et al. Int J Oncol. 2015, 47(2):764-72.
[2] Kridel SJ, et al. Cancer Res. 2004, 64(6):2070-5.

化學(xué)信息&溶解度

分子量	495.73	分子式	C₂₉H₅₃NO₅
CAS號	96829-58-2	SDF	Download Orlistat SDF
Smiles	CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (201.72 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 100 mg/mL (201.72 mM)

Water : Insoluble

DMSO : 99 mg/mL ( (199.7 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 99 mg/mL (199.7 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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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):

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