Catalog No.S1629 Synonyms: Ro 18-0647, Tetrahydrolipstatin
Molecular Weight(MW): 495.73
Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice.
Purity & Quality Control
Choose Selective Lipase Inhibitors
|Description||Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice.|
Orlistat, an inhibitor of lipases and fatty acid synthase, is used orally for long-term treatment of obesity. Orlistat shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein.
|In vivo||Orlistat, administered by oral route, is minimally absorbed by the gastrointestinal tract and is able to prevent the absorption of a large percentage of lipids, thereby reducing lipid supply from outside sources. Because of its extremely low oral bioavailability, the effects of Orlistat are largely confined to the gastrointestinal tract, where it inactivates pancreatic lipase. Therefore, the formulation and route of delivery would have to be changed to treat tumors of the breast, prostate, and so on. Orlistat halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice. A pharmacokinetic analysis of Orlistat (155 mg/kg) administered by i.p. injection showed peak blood levels to be ∼10 μM 2 h after dosing (data not shown). Beyond this time, blood levels of the drug decayed rapidly.|
|In vitro||DMSO||99 mg/mL (199.7 mM)|
|Ethanol||99 mg/mL (199.7 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+corn oil
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Ro 18-0647, Tetrahydrolipstatin|
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01755676||Recruiting||Obesity||EMS||September 2016||Phase 3|
|NCT02767531||Recruiting||Hyperlipoproteinemia Type I|Hypertriglyceridemia||University of Texas Southwestern Medical Center||December 2015||Phase 2|
|NCT01675154||Recruiting||Type 1 Hyperlipoproteinemia||University of Texas Southwestern Medical Center||November 2015||Phase 2|
|NCT02432209||Recruiting||Infertility, Female||Yale University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|Penn State University|Augusta University|University of California, San Francisco|University of North Carolina|University of Oklahoma|University of Pennsylvania||August 2015||Early Phase 1|
|NCT02069197||Recruiting||Obesity|Diabetes|Obstructive Sleep Apnea||Mid-Atlantic Epilepsy and Sleep Center, LLC||January 2014||Phase 2|
|NCT01597531||Unknown status||Type 2 Diabetes|Gastric Banding||East Carolina University||June 2012||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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