1. Metabolic Enzyme/Protease Apoptosis
  2. Fatty Acid Synthase (FASN) Apoptosis
  3. Orlistat

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

Cat. No.: HY-B0218 Purity: 98.42%
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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

Orlistat Chemical Structure

CAS No. : 96829-58-2

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10 mM * 1 mL in DMSO
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500 mg USD 229 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Orlistat:

Top Publications Citing Use of Products

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    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.
    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)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 98.42%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      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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    Product Name:
    Orlistat
    Cat. No.:
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