Orlistat (Synonyms: Tetrahydrolipstatin; Ro-18-0647)

Name: Orlistat
Brand: MedChemExpress
SKU: HY-B0218
Rating: 5.0 (15 reviews)

Cat. No.: HY-B0218 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

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Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity. Anti-atherosclerotic effect.

For research use only. We do not sell to patients.

Orlistat Chemical Structure

CAS No. : 96829-58-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 103	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 229	In-stock	Estimated Time of Arrival: December 31
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5 g		Get quote

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Based on 15 publication(s) in Google Scholar

Other Forms of Orlistat:

Orlistat-d₃ Get quote
Orlistat (Standard) Get quote

14 Publications Citing Use of MCE Orlistat

: Orlistat purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Mar 15;10(3). pii: E353. [Abstract]; Treatment with Orlistat leads to increased phospho-ACC without affecting the phosphorylation status of TOPK/survivin.

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	8.45 μM Compound: Orlistat	Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay	[PMID: 25513712]
COS-7	IC₅₀	1 μM Compound: 1, THL	Inhibition of human recombinant DAGL-alpha-mediated sn-1-[14C]oleoyl-2-arachidonoyl-glycerol hydrolysis to 2-AG overexpressed in african green monkey COS7 cell membrane by scintillation counting Inhibition of human recombinant DAGL-alpha-mediated sn-1-[14C]oleoyl-2-arachidonoyl-glycerol hydrolysis to 2-AG overexpressed in african green monkey COS7 cell membrane by scintillation counting	[PMID: 18831576]
HEK293	IC₅₀	0.19 μM Compound: THL, orlistat	Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method	[PMID: 26344596]
HEK-293T	IC₅₀	> 100 μM Compound: THL	Inhibition of recombinant KIAA1363 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant KIAA1363 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	> 100 μM Compound: THL	Inhibition of recombinant FAAH transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant FAAH transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	0.03 μM Compound: THL	Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	0.05 μM Compound: THL	Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	0.08 μM Compound: THL	Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	10 nM Compound: 3, THL	Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay	[PMID: 22738638]
HepG2	EC₅₀	28.2 μM Compound: Orlistat	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
MCF7	IC₅₀	> 1 x 10⁵ nM Compound: 1; THL	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29541373]
MDA-MB-231	IC₅₀	> 1 x 10⁵ nM Compound: 1; THL	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29541373]
MDA-MB-435	IC₅₀	16.8 μM Compound: orlistat	Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay	[PMID: 18710210]
NCI-H460	IC₅₀	> 1 x 10⁵ nM Compound: 1; THL	Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29541373]
PANC-1	IC₅₀	203 μM Compound: Orlistat	Inhibition of FASN in human PANC1 cells assessed as inhibition of [14C]acetate incorporation preincubated for 4 hrs before [14C]acetate addition measured after 2 hrs by scintillation counting Inhibition of FASN in human PANC1 cells assessed as inhibition of [14C]acetate incorporation preincubated for 4 hrs before [14C]acetate addition measured after 2 hrs by scintillation counting	[PMID: 25513712]

In Vitro

Orlistat (40 μM; 2 days) does not affect MGMT levels in a human melanoma cell line, but downregulates the repair protein by 30-70% in human peripheral blood mononuclear cells, in two leukemia and two colon cancer cell lines. Orlistat does not alter noticeably MGMT mRNA expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	The human melanoma cell line M10, Peripheral blood mononuclear cells , The human Jurkat CD4⁺ T cell leukemia cell line, the human promyelocytic leukemia cell line HL-60, the epithelial colon cancer HCT116 cells,non adherent mononuclear cells (NAMNC)^[1]
Concentration:	2.5, 5, 10, 20, 40 μM for Jurkat cells; 20 and 40 μM for HCT116 cells; 40 μM for normal NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, and HT-29 colon cancer cells
Incubation Time:	2 days for Jurkat cells; 2 or 4 days for HCT116 cells; 2 days for NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, HT-29 colon cancer
Result:	Reduced by >50% the MGMT level at the concentration of 40 μM for Jurkat cells, whereas little or no effect was found when lower concentrations were used. Downregulation of MGMT expression is produced at 40 μM for HCT116 cells. Provoked an ~50% reduction of MGMT level at 40 μM in normal NAMNC, and HL-60 promyelocytic leukemia, HT-29 colon cancer cells except for melanoma M10 cells that showed no downregulation of the protein.

In Vivo

Orlistat (10 mg/kg/day) significantly improves lipid profile, increases antioxidant enzymes and expression of anti-inflammatory markers, and decreases the expression of the pro-inflammatory marker compared to the obese (OB) group^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Eighteen male rats of Sprague–Dawley strain aged between 8–10 weeks weighing 200-250 g^[2]
Dosage:	10 mg/kg/day
Administration:	Orally; six weeks
Result:	Treatment persistently restored the increased body weight, which was significantly observed at the ninth week until the end of the experimental period.

Clinical Trial

Molecular Weight

495.73

Formula

C₂₉H₅₃NO₅

CAS No.

96829-58-2

Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@@H](CCCCCC)[C@H](C[C@@H](OC([C@@H](N([H])C([H])=O)CC(C)C)=O)CCCCCCCCCCC)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (201.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0172 mL	10.0861 mL	20.1723 mL
5 mM	0.4034 mL	2.0172 mL	4.0345 mL
10 mM	0.2017 mL	1.0086 mL	2.0172 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.04 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (251 KB) HNMR (289 KB) RP-HPLC (211 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Giorgia Cioccoloni, et al. Influence of fatty acid synthase inhibitor orlistat on the DNA repair enzyme O6-methylguanine-DNA methyltransferase in human normal or malignant cells in vitro. Int J Oncol. 2015 Aug;47(2):764-72. [Content Brief]

[2]. Zaidatul Akmal Othman, et al. Anti-Atherogenic Effects of Orlistat on Obesity-Induced Vascular Oxidative Stress Rat Model. Antioxidants (Basel). 2021 Feb 6;10(2):251. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0172 mL	10.0861 mL	20.1723 mL	50.4307 mL
	5 mM	0.4034 mL	2.0172 mL	4.0345 mL	10.0861 mL
	10 mM	0.2017 mL	1.0086 mL	2.0172 mL	5.0431 mL
	15 mM	0.1345 mL	0.6724 mL	1.3448 mL	3.3620 mL
	20 mM	0.1009 mL	0.5043 mL	1.0086 mL	2.5215 mL
	25 mM	0.0807 mL	0.4034 mL	0.8069 mL	2.0172 mL
	30 mM	0.0672 mL	0.3362 mL	0.6724 mL	1.6810 mL
	40 mM	0.0504 mL	0.2522 mL	0.5043 mL	1.2608 mL
	50 mM	0.0403 mL	0.2017 mL	0.4034 mL	1.0086 mL
	60 mM	0.0336 mL	0.1681 mL	0.3362 mL	0.8405 mL
	80 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6304 mL
	100 mM	0.0202 mL	0.1009 mL	0.2017 mL	0.5043 mL

Orlistat Related Classifications

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Orlistat (Synonyms: Tetrahydrolipstatin; Ro-18-0647)

Customer Review

Other Forms of Orlistat:

14 Publications Citing Use of MCE Orlistat

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Orlistat (Synonyms: Tetrahydrolipstatin; Ro-18-0647)

Customer Review

Other Forms of Orlistat:

Orlistat Related Antibodies

14 Publications Citing Use of MCE Orlistat

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References

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Orlistat Related Antibodies

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Complete Stock Solution Preparation Table

Orlistat Related Classifications

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