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50mg |
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250mg |
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Purity: ≥98%
Orlistat (also known as tetrahydrolipstatin, or Ro 18-0647, Lipase Inhibitor, THL ) is a potent and general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat is a drug designed to treat obesity. Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. Mechanistic studies suggest that Orlistat inhibits the thioesterase domain of fatty acid synthase (FAS) and as a result halts cell proliferation and causes cell apoptosis. More detailed experiments show that gradually Orlistat affects the retinoblastoma protein pathway and leads to cell-cycle arrest at G1/S boundary.
ln Vitro |
Orlistat (40 μM; 2 days) invoiced repair proteins by 30-70% in human peripheral blood mononuclear cells, two leukocytes, and another Turkish line, but had no effect on MGMT levels in human melanoma cell lines.
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ln Vivo |
Orlistat (10 mg/kg/day) considerably improved blood lipid profile, upregulated antioxidant enzyme expression and anti-inflammatory marker expression, and downregulated pro-inflammatory marker expression as compared to the nutrition (OB) group [2].
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Cell Assay |
Western Blot analysis [1]
Cell Types: human melanoma cell line M10, peripheral blood mononuclear cells, human Jurkat CD4+ T cell leukemia cell line, human promyelocytic leukemia cell line HL-60. Will Dramatically change MGMT mRNA expression [1]. , epithelial colon cancer HCT116 cells, non-adherent mononuclear cells (NAMNC) [1] Tested Concentrations: 2.5, 5, 10, 20, 40 μM for Jurkat cells; 20 and 40 μM for HCT116 cells; normal NAMNC, M10 melanoma , 40 μM for HL-60 promyelocytic leukemia and HT-29 colon cancer cells. Incubation Duration: 2 days for Jurkat cells; 2 or 4 days for HCT116 cells; NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, HT-29 colon cancer 2-day Experimental Results: For Jurkat cells, MGMT levels were diminished by >50% at a concentration of 40 μM, whereas at lower concentrations, almost no effect was seen. used. MGMT expression in HCT116 cells was downregulated at 40 μM. At a concentration of 40 μM, MGMT levels were diminished by approximately 50% in normal NAMNC, HL-60 promyelocytic leukemia, a |
Animal Protocol |
Animal/Disease Models: Eighteen male SD (SD (Sprague-Dawley)) strain rats, aged 8-10 weeks, weighing 200-250 g[2]
Doses: 10 mg/kg/day Doses: po (po (oral gavage)) Six-week Experimental Results: Treatment There was a sustained recovery of the gained weight, which was observed Dramatically from the ninth week until the end of the experimental period. |
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.
[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. |
Molecular Formula |
C29H53NO5
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Molecular Weight |
495.73
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CAS # |
96829-58-2
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Related CAS # |
Orlistat (Standard);96829-58-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O1C([C@@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])[C@]1([H])C([H])([H])[C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])OC([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([H])=O)=O)=O
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InChi Key |
AHLBNYSZXLDEJQ-FWEHEUNISA-N
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InChi Code |
InChI=1S/C29H53NO5/c1-5-7-9-11-12-13-14-15-16-18-24(34-29(33)26(30-22-31)20-23(3)4)21-27-25(28(32)35-27)19-17-10-8-6-2/h22-27H,5-21H2,1-4H3,(H,30,31)/t24-,25-,26-,27-/m0/s1
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Chemical Name |
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-4-methylpentanoate
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.04 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.