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Orlistat

Name: Orlistat
Brand: TargetMol
SKU: T0686
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0686Cas No. 96829-58-2

Alias Tetrahydrolipstatin, Ro-18-0647

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Orlistat

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Purity: 99.86%

Catalog No. T0686Alias Tetrahydrolipstatin, Ro-18-0647Cas No. 96829-58-2

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$30	In Stock	In Stock
50 mg	$38	In Stock	In Stock
100 mg	$52	In Stock	In Stock
500 mg	$133	In Stock	In Stock
1 g	$193	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.86%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Orlistat AI Summary

Orlistat demonstrates significant inhibitory activity against multiple enzymes involved in lipid metabolism and signaling pathways. It effectively inhibits porcine pancreatic lipase, showing IC50 values ranging from 220.0 nM to 600.0 nM, and exhibits antihyperlipidemic and potential antiobesity effects in various animal models. Additionally, Orlistat shows binding affinity for cannabinoid receptor 1 (IC50 ≤ 100.0 nM) and inhibits fatty acid synthase thioesterase domain (IC50 of 1350.0 nM). It also demonstrates cytotoxicity against human MDA-MB-435 cells with an IC50 of 16800.0 nM, while its inhibition of other key enzymes, such as human recombinant DAGL-alpha, ABHD12, and phospholipases, highlights its diverse bioactivity. Moreover, Orlistat shows antiviral activity against SARS-CoV-2 and Mycobacterium tuberculosis, and inhibits ABHD6 (IC50 of 48.0 nM). Notably, the compound also exhibits cytotoxic effects in various cell lines at different concentrations. Furthermore, it demonstrates potential liver toxicity with a DILI severity score of 8.0. These findings suggest the compound's potential therapeutic applications in lipid metabolism disorders, obesity, and infectious diseases, with careful consideration needed for its cytotoxic and hepatotoxic properties..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.
In vitro	METHODS: Prostate cancer cells PC3, DU145 and LNCaP were treated with Orlistat (10-300 µM) for 24 h and cell proliferation was detected by MTT assay. RESULTS: Increasing concentrations of Orlistat resulted in a dose-dependent decrease in cell viability of the three PCa cell lines tested. [1] METHODS: Breast cancer cells SK-Br3 were treated with Orlistat (40 µM) for 6-72 h. Cell cycle was measured by Flow cytometry. RESULTS: The time-dependent response of SK-Br3 breast cancer cells to Orlistat was characterized by the absence of G2-M populations and the accumulation of cells in the S phase of the cell cycle. Importantly, Orlistat exposure significantly promoted apoptosis, as evidenced by the time-dependent accumulation of sub-G1 populations with <2N DNA and representing dead cells. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, Orlistat (240 mg/kg, 33% ethanol and 66% PEG 400) was injected intraperitoneally into athymic nude mice bearing PC-3 xenografts once daily for three weeks. RESULTS: Orlistat prevented PC-3 tumor growth. In five separate experiments, tumor growth was blocked by 63%, 62%, 46%, 41%, and 16%. [3]
Synonyms	Tetrahydrolipstatin, Ro-18-0647

Chemical Properties

Molecular Weight	495.73
Formula	C₂₉H₅₃NO₅
Cas No.	96829-58-2
Smiles	C([C@@H](OC([C@H](CC(C)C)NC=O)=O)CCCCCCCCCCC)[C@H]1[C@H](CCCCCC)C(=O)O1
Relative Density.	0.976 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 260 mg/mL (524.48 mM), Sonication is recommended.

Ethanol: 49.6 mg/mL (100.05 mM), Sonication is recommended.

In Vivo Formulation

33% Ethanol + 67% PEG 400/PEG 300: 10 mg/mL (20.17 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0172 mL	10.0861 mL	20.1723 mL	100.8614 mL
5 mM	0.4034 mL	2.0172 mL	4.0345 mL	20.1723 mL
10 mM	0.2017 mL	1.0086 mL	2.0172 mL	10.0861 mL
20 mM	0.1009 mL	0.5043 mL	1.0086 mL	5.0431 mL
50 mM	0.0403 mL	0.2017 mL	0.4034 mL	2.0172 mL
100 mM	0.0202 mL	0.1009 mL	0.2017 mL	1.0086 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Orlistat

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