Orlistat
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 495.73 |
| Cas No. | 96829-58-2 |
| Formula | C29H53NO5 |
| Solubility | insoluble in H2O; ≥17.4 mg/mL in DMSO; ≥26.8 mg/mL in EtOH |
| Chemical Name | [(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-4-methylpentanoate |
| SDF | Download SDF |
| Canonical SMILES | CCCCCCCCCCCC(CC1C(C(=O)O1)CCCCCC)OC(=O)C(CC(C)C)NC=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Jurkat CD4+ T cell leukemia cell line |
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Preparation method |
The solubility of this compound in DMSO is > 17.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
2.5, 5, 10, 20 or 40 μM; 1 ~ 3 days |
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Applications |
In Jurkat CD4+ T cell leukemia cell line, Orlistat, at the concentration of 40 μM, reduced O6-methylguanine-DNA methyltransferase (MGMT) expression by > 50% on day 2, whereas little or no effect was observed when lower concentrations were applied. The effect of Orlistat persisted on day 3. However, on day 1, Orlistat did not remarkably change the MGMT level. |
| Animal experiment [2]: | |
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Animal models |
Nude mice bearing PC-3 tumors |
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Dosage form |
155 mg/kg or 240 mg/kg/day; i.p. |
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Applications |
In nude mice bearing PC-3 tumors, Orlistat at the dose of 240 mg/kg/day inhibited tumor growth and induced tumor cell apoptosis. A pharmacokinetic study of Orlistat (155 mg/kg) administered by i.p. injection showed the peak blood level of Orlistat (~10 μM) achieved 2 hrs after dosing. After 2hrs, the blood level of Orlistat decreased rapidly. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Cioccoloni G, Bonmassar L, Pagani E, Caporali S, Fuggetta MP, Bonmassar E, D'Atri S, Aquino A. 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. [2]. Kridel SJ, Axelrod F, Rozenkrantz N, Smith JW. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity. Cancer Res. 2004 Mar 15;64(6):2070-5. | |
Quality Control & MSDS
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Chemical structure
