Catalog No.S1629 Synonyms: Ro 18-0647, Tetrahydrolipstatin

Orlistat  Chemical Structure

Molecular Weight(MW): 495.73

Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 270 In stock
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Biological Activity

Description Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice.
lipase [1]
(Cell-free assay)
Fatty acid synthesis [1]
(Cell-free assay)
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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T cell NFjXd5FHfW6ldHnvckBie3OjeR?= MlPPTY5pcWKrdHnvckBw\iCqdX3hckBFSUeOYXzwbIEh\XiycnXzd4VlKGmwIFjFT|I6O1RiY3XscEBu\W2kcnHu[UB2e2mwZzDbNVREZVODRzDzeYJ{fHKjdHWgbY4h\GW2ZYLn[Y51KG[{ZXWgd49tfXSrb36gZpkhTlKHVDDhd5NigSxiSVO1NF0xNjBzIN88US=> NETVc2IzOjd|OE[zPC=>
COS7 cells NXPxTmlOTnWwY4Tpc44h[XO|YYm= NWLwd4pmUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDERWdN[WyyaHGgc5ZmemW6cILld5Nm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{NCCLQ{WwQVAvODZizszN MXSxPFY2Pzl5MR?=
MDA-MB-435 cells Mn3BR5l1d3SxeHnjbZR6KGG|c3H5 NEfrOog1QCCq Mo\QR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscEB1cXSncjDhd5NigSxiSVO1NF0yPi56IN88US=> NGPuT2kyQDdzMEKxNC=>
HepG2 (DPX-2) cells NXywUldQTnWwY4Tpc44h[XO|YYm= Ml7MNlQhcA>? NHTGNY9C[3SrdnH0bY9vKG:oIHj1cYFvKFC[UjDlfJBz\XO|ZXSgbY4hcHWvYX6gTIVxTzJiKFTQXE0zMSClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gR3lRO0F2IHHmeIVzKDJ2IHjyd{BjgSCudX3pcoV{[2WwdDDhcoFtgXOrczygSWM2OD1{OD6yJO69VQ>? Ml;kNlA6PjZyNEO=

... Click to View More Cell Line Experimental Data

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].


Cell Research:


+ Expand
  • 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.

    (Only for Reference)
Animal Research:


+ Expand
  • Animal Models: Nude mice (PC-3 xenograft tumor)
  • Formulation: 33% ethanol and 66% PEG 400
  • Dosages: 240 mg/kg/day
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL (199.7 mM)
Ethanol 99 mg/mL (199.7 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
5% DMSO+corn oil
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 495.73


CAS No. 96829-58-2
Storage powder
in solvent
Synonyms Ro 18-0647, Tetrahydrolipstatin

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01755676 Recruiting Obesity EMS September 2016 Phase 3
NCT02767531 Recruiting Hyperlipoproteinemia Type I|Hypertriglyceridemia University of Texas Southwestern Medical Center December 2015 Phase 2
NCT01675154 Recruiting Type 1 Hyperlipoproteinemia University of Texas Southwestern Medical Center November 2015 Phase 2
NCT02432209 Recruiting Infertility, Female Yale University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|Penn State University|Augusta University|University of California, San Francisco|University of North Carolina|University of Oklahoma|University of Pennsylvania August 2015 Early Phase 1
NCT02069197 Recruiting Obesity|Diabetes|Obstructive Sleep Apnea Mid-Atlantic Epilepsy and Sleep Center, LLC January 2014 Phase 2
NCT01597531 Unknown status Type 2 Diabetes|Gastric Banding East Carolina University June 2012 Phase 4

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID