Name: Orlistat
Brand: Selleck Chemicals
SKU: S1629
Rating: 5 (14 reviews)

Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.

Orlistat Chemical Structure

CAS: 96829-58-2

Selleck's Orlistat has been cited by 14 publications

Purity & Quality Control

Batch: Purity: 99.98%

99.98

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Choose Selective Lipase Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
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
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
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
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
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
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
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	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
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
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
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		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			Inhibition of human ABHD12 containing pCMV6-XL4-hABHD12 transfected into HEK293 cells, IC50 = 0.19055 μM.	25752982
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
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
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-231	Cytotoxicity assay			Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability, IC50 = 13 μM.	29541373
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
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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description

Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.

Targets

lipase ^[1]
(Cell-free assay)

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

In vitro
In vitro	Orlistat, an inhibitor of lipases and fatty acid synthase, is used orally for long-term treatment of obesity. Orlistat shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein^[1].
Cell Research	Cell lines	Jurkat CD4+ T cell leukemia cell line
	Concentrations	2.5, 5, 10, 20, 40 μM
	Incubation Time	2 days
	Method	Leukemic cells were cultured in the presence of graded concentrations of orlistat for two days. Control cultures were exposed to DMSO alone at the concentration corresponding to that utilized for orlistat 40 μM. At the end of the in vitro treatment, leukemic cells were lysed and subjected to western blot (WB) analysis.
Experimental Result Images	Methods	Biomarkers	Images	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

In Vivo
In vivo	Orlistat, administered by oral route, is minimally absorbed by the gastrointestinal tract and is able to prevent the absorption of a large percentage of lipids, thereby reducing lipid supply from outside sources^[1]. Because of its extremely low oral bioavailability, the effects of Orlistat are largely confined to the gastrointestinal tract, where it inactivates pancreatic lipase. Therefore, the formulation and route of delivery would have to be changed to treat tumors of the breast, prostate, and so on. Orlistat halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice. A pharmacokinetic analysis of Orlistat (155 mg/kg) administered by i.p. injection showed peak blood levels to be ∼10 μM 2 h after dosing (data not shown). Beyond this time, blood levels of the drug decayed rapidly^[2].
Animal Research	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

Chemical Information & Solubility

Molecular Weight	495.73	Formula	C₂₉H₅₃NO₅
CAS No.	96829-58-2	SDF	Download Orlistat SDF
Smiles	CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 99 mg/mL ( (199.7 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 99 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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