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Orlistat [96829-58-2]

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Referencia HY-B0218-200mg

embalaje : 200mg

Contact local distributor :

Teléfono : +1 850 650 7790

Marca : MedChemExpress

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Contact local distributor :

Teléfono : +1 850 650 7790

Descripciòn

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^[1]. Anti-atherosclerotic effect^[2].

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.

Ensayo clínico

Peso molecular

495.73

Fòrmula

C₂₉H₅₃NO₅

No. CAS

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(13)C(13)=O)CC(C)C)=O)CCCCCCCCCCC)O1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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.

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.

Pureza y Documentación

Purity: 99.97%

Ficha de datos (280 KB) SDS (393 KB)

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

Instrucciones de manejo (2659 KB)

Referencias

[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]

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Referencia HY-B0218-200mg

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

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