For research use only.

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

1 publication

Orlistat Chemical Structure

CAS No. 96829-58-2

Orlistat (Ro 18-0647, Tetrahydrolipstatin) 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.

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Selleck's Orlistat has been cited by 1 publication

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Biological Activity

Description Orlistat (Ro 18-0647, Tetrahydrolipstatin) 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.
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 M1\3cGZ2dmO2aX;uJIF{e2G7 NYqwZ215UW6qaXLpeIlwdiCxZjDoeY1idiCGQVfMZYxxcGFiZYjwdoV{e2WmIHnuJGhGUzJ7M2SgZ4VtdCCvZX3idoFv\SC3c3nu[{BcOTSFXWPBS{B{fWK|dILheIUhcW5iZHX0[ZJo\W62IH\y[YUhe2:udYTpc44h[nliRmLFWEBie3OjeTygTWM2OD1yLkCxJO69VQ>? NXLYNYhkOjJ5M{i2N|g>
COS7 cells MYLGeY5kfGmxbjDhd5NigQ>? NUHmPXFzUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDERWdN[WyyaHGgc5ZmemW6cILld5Nm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{NCCLQ{WwQVAvODZizszN M3Lz[VE5PjV5OUex
MDA-MB-435 cells M2PC[2N6fG:2b4jpZ4l1gSCjc4PhfS=> NULPWmtLPDhiaB?= NYnDW4dTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdCC2aYTldkBie3OjeTygTWM2OD1zNj64JO69VQ>? M{jrZlE5PzFyMkGw
HepG2 (DPX-2) cells M160WWZ2dmO2aX;uJIF{e2G7 NFLwdW4zPCCq NH;vPJFC[3SrdnH0bY9vKG:oIHj1cYFvKFC[UjDlfJBz\XO|ZXSgbY4hcHWvYX6gTIVxTzJiKFTQXE0zMSClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gR3lRO0F2IHHmeIVzKDJ2IHjyd{BjgSCudX3pcoV{[2WwdDDhcoFtgXOrczygSWM2OD1{OD6yJO69VQ>? MmfVNlA6PjZyNEO=

... Click to View More Cell Line Experimental Data

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. 

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.

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:


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  • 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:


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

Solubility (25°C)

In vitro DMSO 99 mg/mL (199.7 mM)
Water Insoluble
Ethanol ''99 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
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 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID